NAV

Nimodipine

Identification

Summary

Nimodipineis a calcium channel blocker used to improve neurological outcomes in patients with subarachnoid hemorrhage due to a ruptured intracranial aneurysm.

Brand Names
Nimotop, Nymalize
Generic Name
Nimodipine
DrugBank Accession Number
DB00393
Background

Nimodipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nimodipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Compared to other calcium channel blocking agents, nimodipine exhibits greater effects on cerebral circulation than on peripheral circulation. Nimodipine is used to as an adjunct to improve the neurologic outcome following subarachnoid hemorrhage from ruptured intracranial aneurysm.

Type
Small Molecule
Groups
Approved, Investigational
Structure
 3D
Similar Structures
Weight
Average: 418.4403
Monoisotopic: 418.174001196
Chemical Formula
C21H26N2O7
Synonyms
  • 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-β-methoxyethyl ester 5-isopropyl ester
  • isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate
  • isopropyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate
  • Nimodipine
  • Nimodipino
  • Nimodipinum
External IDs
  • BAY E 9736
  • BAY-E-9736

Pharmacology

Indication

For use as an adjunct to improve neurologic outcome following subarachnoid hemorrhage (SAH) from ruptured intracranial berry aneurysms by reducing the incidence and severity of ischemic deficits.

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
Improve clinical decision support with information oncontraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

Nimodipine属于一类药物agents known as calcium channel blockers. Nimodipine is indicated for the improvement of neurological outcome by reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from ruptured congenital aneurysms who are in good neurological condition post-ictus (e.g., Hunt and Hess Grades I-III). The contractile processes of smooth muscle cells are dependent upon calcium ions, which enter these cells during depolarization as slow ionic transmembrane currents. Nimodipine inhibits calcium ion transfer into these cells and thus inhibits contractions of vascular smooth muscle. In animal experiments, nimodipine had a greater effect on cerebral arteries than on arteries elsewhere in the body perhaps because it is highly lipophilic, allowing it to cross the blood brain barrier.

Mechanism of action

Although the precise mechanism of action is not known, nimodipine blocks intracellular influx of calcium through voltage-dependent and receptor-operated slow calcium channels across the membranes of myocardial, vascular smooth muscle, and neuronal cells. By specifically binding to L-type voltage-gated calcium channels, nimodipine inhibits the calcium ion transfer, resulting in the inhibition of vascular smooth muscle contraction. Evidence suggests that the dilation of small cerebral resistance vessels, with a resultant increase in collateral circulation, and/or a direct effect involving the prevention of calcium overload in neurons may be responsible for nimodipine's clinical effect in patients with subarachnoid hemorrhage.

Target Actions Organism
AVoltage-dependent L-type calcium channel subunit alpha-1C
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit alpha-1D
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit alpha-1F
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit alpha-1S
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit beta-1
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit beta-2
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit beta-3
inhibitor
 Humans
AVoltage-dependent L-type calcium channel subunit beta-4
inhibitor
 Humans
UMineralocorticoid receptor
antagonist
 Humans
UAryl hydrocarbon receptor
agonist
 Humans
Absorption

In humans, nimodipine is rapidly absorbed after oral administration, and peak concentrations are generally attained within one hour. Bioavailability is 100% following intravenous administration and 3-30% following oral administration due to extensive first-pass metabolism.

Volume of distribution

Not Available

Protein binding

95% bound to plasma protein

Metabolism

Hepatic metabolism via CYP 3A4.

Route of elimination

Nimodipine is eliminated almost exclusively in the form of metabolites and less than 1% is recovered in the urine as unchanged drug. Numerous metabolites, all of which are either inactive or considerably less active than the parent compound, have been identified.

Half-life

1.7-9 hours

Clearance

Not Available

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including:blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Symptoms of overdosage would be expected to be related to cardiovascular effects such as excessive peripheral vasodilation with marked systemic hypotension.

Pathways
Pathway Category
Nimodipine Action Pathway Drug action
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction
Integrate drug-drug
interactions in your software
Abaloparatide The risk or severity of adverse effects can be increased when Nimodipine is combined with Abaloparatide.
Abametapir The serum concentration of Nimodipine can be increased when it is combined with Abametapir.
Acarbose The risk or severity of hypoglycemia can be increased when Nimodipine is combined with Acarbose.
Acebutolol Nimodipine may increase the arrhythmogenic activities of Acebutolol.
Aceclofenac The therapeutic efficacy of Nimodipine can be decreased when used in combination with Aceclofenac.
Acemetacin The therapeutic efficacy of Nimodipine can be decreased when used in combination with Acemetacin.
Acetohexamide The risk or severity of hypoglycemia can be increased when Nimodipine is combined with Acetohexamide.
Acetyldigitoxin Nimodipine may increase the arrhythmogenic activities of Acetyldigitoxin.
Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Nimodipine.
Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nimodipine.
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
  • Avoid grapefruit products.
  • Take with or without food. Take consistently at the same time in regard to meals.

Products

Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Product Images
International/Other Brands
Periplum
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Nimotop Capsule, gelatin coated 30 mg/1 Oral Bayer 1988-12-28 2009-04-30 美国国旗
Nimotop Tablet 30 mg Oral Bayer 2009-07-24 Not applicable Canada flag
Nimotop - Cap 30mg Capsule 30 mg Oral Bayer 1989-12-31 2009-08-06 Canada flag
Nimotop Cap 30mg Capsule 30 mg Oral Miles Canada Inc. Pharmaceutical Division 1989-12-31 1996-10-02 Canada flag
Nimotop I.V.-0.2mg/ml Liquid .2 mg / mL Intravenous Bayer 1996-10-08 2000-09-19 Canada flag
Nimotop IV 0.2mg/ml Liquid 0.2 mg / mL Intravenous Miles Canada Inc. Pharmaceutical Division 1992-12-31 2000-08-01 Canada flag
Nymalize Solution 30 mg/10mL Oral Arbor Pharmaceuticals 2017-04-06 Not applicable 美国国旗
Nymalize Solution 30 mg/5mL Oral Azurity Pharmaceuticals, Inc. (formerly Arbor Pharmaceuticals) 2020-05-04 Not applicable 美国国旗
Nymalize Solution 60 mg/20mL Oral Arbor Pharmaceuticals 2013-06-03 Not applicable 美国国旗
Nymalize Solution 60 mg/10mL Oral Azurity Pharmaceuticals, Inc. (formerly Arbor Pharmaceuticals) 2020-05-04 Not applicable 美国国旗
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Nimodipine Capsule, liquid filled 30 mg/1 Oral Barr Laboratories 2007-05-25 2014-06-30 美国国旗
Nimodipine Capsule 30 mg/1 Oral ANI Pharmaceuticals, Inc. 2015-11-01 2022-09-30 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral American Health Packaging 2015-02-17 2023-09-30 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral Cardinal Health 2008-03-21 Not applicable 美国国旗
Nimodipine Capsule 30 mg/1 Oral Cardinal Health 2007-06-28 2013-07-31 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral Bionpharma Inc. 2017-11-21 Not applicable 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral 传统制药公司。 2008-03-21 Not applicable 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral Major 2015-01-01 2019-12-16 美国国旗
Nimodipine Capsule, liquid filled 30 mg/1 Oral 传统制药公司。d/b/a Avet Pharmaceuticals Inc. 2017-11-07 Not applicable 美国国旗
Nimodipine Capsule 30 mg/1 Oral Sun Pharmaceutical Industries, Inc. 2007-06-28 2011-12-31 美国国旗

Categories

ATC Codes
C08CA06 — Nimodipine
Drug Categories
Chemical TaxonomyProvided byClassyfire
Description
This compound belongs to the class of organic compounds known as dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Hydropyridines
Direct Parent
Dihydropyridinecarboxylic acids and derivatives
Alternative Parents
Nitrobenzenes/Nitroaromatic compounds/Dicarboxylic acids and derivatives/Vinylogous amides/Enoate esters/Amino acids and derivatives/Propargyl-type 1,3-dipolar organic compounds/Azacyclic compounds/Dialkyl ethers/Dialkylamines
show 7 more
Substituents
Allyl-type 1,3-dipolar organic compound/Alpha,beta-unsaturated carboxylic ester/Amine/Amino acid or derivatives/Aromatic heteromonocyclic compound/Azacycle/Benzenoid/C-nitro compound/Carbonyl group/Carboxylic acid derivative
show 25 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
C-nitro compound, diester, dihydropyridine (CHEBI:7575)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
57WA9QZ5WH
CAS number
66085-59-4
InChI Key
UIAGMCDKSXEBJQ-UHFFFAOYSA-N
InChI
InChI = 1 s / C21H26N2O7 c1-12 (2) 30 21 (25) 18-14 (4) 22-13(3)17(20(24)29-10-9-28-5)19(18)15-7-6-8-16(11-15)23(26)27/h6-8,11-12,19,22H,9-10H2,1-5H3
IUPAC Name
3-(2-methoxyethyl) 5-propan-2-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
COCCOC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC(C)C

References

一般引用
  1. Janjua N, Mayer SA: Cerebral vasospasm after subarachnoid hemorrhage. Curr Opin Crit Care. 2003 Apr;9(2):113-9. [Article]
  2. Allen GS, Ahn HS, Preziosi TJ, Battye R, Boone SC, Boone SC, Chou SN, Kelly DL, Weir BK, Crabbe RA, Lavik PJ, Rosenbloom SB, Dorsey FC, Ingram CR, Mellits DE, Bertsch LA, Boisvert DP, Hundley MB, Johnson RK, Strom JA, Transou CR: Cerebral arterial spasm--a controlled trial of nimodipine in patients with subarachnoid hemorrhage. N Engl J Med. 1983 Mar 17;308(11):619-24. [Article]
  3. Belfort MA, Anthony J, Saade GR, Allen JC Jr: A comparison of magnesium sulfate and nimodipine for the prevention of eclampsia. N Engl J Med. 2003 Jan 23;348(4):304-11. [Article]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  5. Tomassoni D, Lanari A, Silvestrelli G, Traini E, Amenta F: Nimodipine and its use in cerebrovascular disease: evidence from recent preclinical and controlled clinical studies. Clin Exp Hypertens. 2008 Nov;30(8):744-66. doi: 10.1080/10641960802580232. [Article]
  6. Vergouwen MD, Vermeulen M, Roos YB: Effect of nimodipine on outcome in patients with traumatic subarachnoid haemorrhage: a systematic review. Lancet Neurol. 2006 Dec;5(12):1029-32. [Article]
  7. FDA Approved Drug Products: Nymalize (nimodipine) oral solution [Link]
Human Metabolome Database
HMDB0014537
KEGG Drug
D00438
KEGG Compound
C07267
PubChem Compound
4497
PubChem Substance
46508497
ChemSpider
4341
BindingDB
50101971
RxNav
7426
ChEBI
7575
ChEMBL
CHEMBL1428
Therapeutic Targets Database
DAP000306
PharmGKB
PA450633
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Nimodipine
FDA label
Download (504 KB)
MSDS
Download (73.3 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Completed Treatment Cerebral Infarctions 1
4 Completed Treatment Dementia 1
4 Suspended Prevention Coronavirus Disease 2019 (COVID‑19)/Hypertension 1
4 Terminated Treatment Depression 1
4 Unknown Status Prevention Cerebrovascular Accident/Mild Cognitive Impairment (MCI) 1
4 Withdrawn Treatment Reversible cerebral vasoconstriction syndrome 1
3 Recruiting Treatment Anticholinesterase Insecticide Poisoning/Poisoning caused by organophosphorus pesticides 1
3 Terminated Treatment Aneurysmal Subarachnoid Hemorrhages (aSAH) 1
2 Active Not Recruiting Treatment Depression/Electroconvulsive Therapy/Epilepsies/Postictal Delirium 1
2 Completed Treatment Cocaine Related Disorders 1

Pharmacoeconomics

Manufacturers
  • Banner pharmacaps inc
  • Barr laboratories inc
  • Sun pharmaceutical industries inc
  • Bayer pharmaceuticals corp
Packagers
  • Amerisource Health Services Corp.
  • Banner Pharmacaps Inc.
  • Barr Pharmaceuticals
  • Bayer Healthcare
  • Caraco Pharmaceutical Labs
  • Cardinal Health
  • Catalent Pharma Solutions
  • Heritage Pharmaceuticals
  • Neuman Distributors Inc.
  • Pharmaceutics International Inc.
  • Sandhills Packaging Inc.
Dosage Forms
Form Route Strength
Tablet, film coated Oral 30 mg
Injection, solution Parenteral 0.2 MG/ML
Solution / drops Oral 30 MG/0.75ML
Capsule Oral 30 mg/1
Capsule, liquid filled Oral 30 mg/1
Solution Intravenous 10 mg
Tablet Oral 30 mg
Capsule, gelatin coated Oral 30 mg/1
Granule, effervescent 30 MG
Injection, solution Parenteral 10 MG/50ML
Solution 0.2 mg/1ml
Tablet, coated Oral 30 mg
Injection Parenteral
Tablet, film coated Oral
Solution Parenteral 50 mg/ml
Capsule Oral 30 mg
Injection Intravenous 0.02 %
Liquid Intravenous .2 mg / mL
Solution Intracisternal; Intravenous
Liquid Intravenous 0.2 mg / mL
Solution Intravenous 0.01 g
Tablet, extended release Oral 120 mg
Suspension Oral 600毫克
Injection Intravenous
Tablet Oral 60 mg
Tablet, extended release Oral 90 mg
Solution Parenteral 10 mg
Solution Oral 30 mg/10mL
Solution Oral 30 mg/5mL
Solution Oral 60 mg/10mL
Solution Oral 60 mg/20mL
Solution Intravenous 0.2 mg
Capsule, coated Oral 90 mg
Granule, effervescent
Solution / drops Oral
Tablet, coated Oral
Injection, solution Parenteral
Prices
Unit description Cost Unit
NiMODipine 100 30 mg capsule Box 952.07USD box
Nimotop 30 mg capsule 9.87USD capsule
Nimodipine 30 mg capsule 9.69USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region
US10342787 No 2019-07-09 2038-04-16 美国国旗
US10576070 No 2020-03-03 2038-04-16 美国国旗
US7070581 No 2006-07-04 2023-06-23 美国国旗
US8517997 No 2013-08-27 2024-05-14 美国国旗
US11207306 No 2021-12-28 2038-04-16 美国国旗
US11413277 No 2018-04-16 2038-04-16 美国国旗
US11517563 No 2018-04-16 2038-04-16 美国国旗

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 125 °C Not Available
logP 3.05 MASUMOTO,K ET AL. (1995)
Predicted Properties
Property Value Source
Water Solubility 0.012 mg/mL ALOGPS
logP 3.41 ALOGPS
logP 2.54 Chemaxon
logS -4.5 ALOGPS
pKa (Strongest Acidic) 16.96 Chemaxon
pKa (Strongest Basic) -4.1 Chemaxon
Physiological Charge 0 Chemaxon
Hydrogen Acceptor Count 6 Chemaxon
Hydrogen Donor Count 1 Chemaxon
Polar Surface Area 117 Å2 Chemaxon
Rotatable Bond Count 10 Chemaxon
Refractivity 111.37 m3·mol-1 Chemaxon
Polarizability 43.07 Å3 Chemaxon
Number of Rings 2 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five Yes Chemaxon
Ghose Filter Yes Chemaxon
Veber's Rule No Chemaxon
MDDR-like Rule No Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9387
Blood Brain Barrier - 0.9358
Caco-2 permeable - 0.5838
P-glycoprotein substrate Substrate 0.752
P-glycoprotein inhibitor I Inhibitor 0.9287
P-glycoprotein inhibitor II Inhibitor 0.9098
Renal organic cation transporter Non-inhibitor 0.8178
CYP450 2C9 substrate Non-substrate 0.8151
CYP450 2D6 substrate Non-substrate 0.9118
CYP450 3A4 substrate Substrate 0.7571
CYP450 1A2 substrate Inhibitor 0.9108
CYP450 2C9 inhibitor Inhibitor 0.8949
CYP450 2D6 inhibitor Non-inhibitor 0.9231
CYP450 2C19 inhibitor Inhibitor 0.8994
CYP450 3A4 inhibitor Inhibitor 0.8248
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8557
Ames test Non AMES toxic 0.5976
Carcinogenicity Non-carcinogens 0.6953
Biodegradation Not ready biodegradable 0.8797
Rat acute toxicity 2.5326 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.6468
hERG inhibition (predictor II) Non-inhibitor 0.8734
ADMET data is predicted usingadmetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
预测MS / MS谱- 20 v -(注释d) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
MS/MS Spectrum - , positive LC-MS/MS splash10-0006-0149000000-2a019013c0386ca13362

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets tounlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Details 1.Voltage-dependent L-type calcium channel subunit alpha-1C
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
分子量
248974.1 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Marchetti C, Usai C: High affinity block by nimodipine of the internal calcium elevation in chronically depolarized rat cerebellar granule neurons. Neurosci Lett. 1996 Mar 29;207(2):77-80. [Article]
  3. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  4. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  5. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  6. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  7. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
  8. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
Details 2.Voltage-dependent L-type calcium channel subunit alpha-1D
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1D
Uniprot ID
Q01668
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1D
分子量
245138.75 Da
References
  1. Sinnegger-Brauns MJ, Huber IG, Koschak A, Wild C, Obermair GJ, Einzinger U, Hoda JC, Sartori SB, Striessnig J: Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms. Mol Pharmacol. 2009 Feb;75(2):407-14. doi: 10.1124/mol.108.049981. Epub 2008 Nov 24. [Article]
  2. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  3. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  5. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  6. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
Details 3.Voltage-dependent L-type calcium channel subunit alpha-1F
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1F
Uniprot ID
O60840
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1F
分子量
220675.9 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  2. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
Details 4.Voltage-dependent L-type calcium channel subunit alpha-1S
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1S
Uniprot ID
Q13698
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1S
分子量
212348.1 Da
References
  1. Peterson BZ, Catterall WA: Allosteric interactions required for high-affinity binding of dihydropyridine antagonists to Ca(V)1.1 Channels are modulated by calcium in the pore. Mol Pharmacol. 2006 Aug;70(2):667-75. Epub 2006 May 4. [Article]
  2. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  3. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  4. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  5. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  6. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
Details 5.Voltage-dependent L-type calcium channel subunit beta-1
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB1
Uniprot ID
Q02641
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-1
分子量
65712.995 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  2. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
Details 6.Voltage-dependent L-type calcium channel subunit beta-2
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB2
Uniprot ID
Q08289
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-2
分子量
73579.925 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
  6. Striessnig, J. (2004). Ca 2+ channel blockers. In Encyclopedic reference of molecular pharmacology (pp. 201-207). Berlin: Springer. [ISBN:9783540298328]
Details 7.Voltage-dependent L-type calcium channel subunit beta-3
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB3
Uniprot ID
P54284
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-3
分子量
54531.425 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  2. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
Details 8.Voltage-dependent L-type calcium channel subunit beta-4
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB4
Uniprot ID
O00305
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-4
分子量
58168.625 Da
References
  1. Weant KA, Ramsey CN 3rd, Cook AM: Role of intraarterial therapy for cerebral vasospasm secondary to aneurysmal subarachnoid hemorrhage. Pharmacotherapy. 2010 Apr;30(4):405-17. doi: 10.1592/phco.30.4.405. [Article]
  2. 董CJ,郭Y,规律的P,惠勒L,兔子佤邦:Nimodipine enhancement of alpha2 adrenergic modulation of NMDA receptor via a mechanism independent of Ca2+ channel blocking. Invest Ophthalmol Vis Sci. 2010 Aug;51(8):4174-80. doi: 10.1167/iovs.09-4613. Epub 2010 Mar 24. [Article]
  3. Kim JH, Park IS, Park KB, Kang DH, Hwang SH: Intraarterial nimodipine infusion to treat symptomatic cerebral vasospasm after aneurysmal subarachnoid hemorrhage. J Korean Neurosurg Soc. 2009 Sep;46(3):239-44. doi: 10.3340/jkns.2009.46.3.239. Epub 2009 Sep 30. [Article]
  4. Kumar R, Mehra R, Ray SB: L-type calcium channel blockers, morphine and pain: Newer insights. Indian J Anaesth. 2010 Mar;54(2):127-31. doi: 10.4103/0019-5049.63652. [Article]
  5. Keyrouz SG, Diringer MN: Clinical review: Prevention and therapy of vasospasm in subarachnoid hemorrhage. Crit Care. 2007;11(4):220. [Article]
Details 9.Mineralocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates targ...
Gene Name
NR3C2
Uniprot ID
P08235
Uniprot Name
Mineralocorticoid receptor
分子量
107066.575 Da
References
  1. Dietz JD, Du S, Bolten CW, Payne MA, Xia C, Blinn JR, Funder JW, Hu X: A number of marketed dihydropyridine calcium channel blockers have mineralocorticoid receptor antagonist activity. Hypertension. 2008 Mar;51(3):742-8. doi: 10.1161/HYPERTENSIONAHA.107.103580. Epub 2008 Feb 4. [Article]
Details 10.Aryl hydrocarbon receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Transcription regulatory region dna binding
Specific Function
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes...
Gene Name
AHR
Uniprot ID
P35869
Uniprot Name
Aryl hydrocarbon receptor
分子量
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [Article]

Enzymes

Details 1.Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
分子量
57342.67 Da
References
  1. Liu XQ, Ren YL, Qian ZY, Wang GJ: Enzyme kinetics and inhibition of nimodipine metabolism in human liver microsomes. Acta Pharmacol Sin. 2000 Aug;21(8):690-4. [Article]
  2. Choi JS, Burm JP: Enhanced nimodipine bioavailability after oral administration of nimodipine with morin, a flavonoid, in rabbits. Arch Pharm Res. 2006 Apr;29(4):333-8. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 24, 2023 03:03