氟立班丝氨的药理学。
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罗德Borsini F,埃文斯K,杰森K, F,亚历山大•B Pollentier年代
氟立班丝氨的药理学。
2002年夏季,中枢神经系统药物启8 (2):117 - 42。
- PubMed ID
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12177684 (在PubMed]
- 文摘
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氟立班丝氨有优惠亲和力血清素5 - (1)、D (4 k)、多巴胺和血清素5 - (2 a)受体。体外microiontophoresis,氟立班丝氨的行为作为一个5 - (1 a)受体激动剂,一个非常弱的部分在多巴胺受体激动剂D(4)受体,和一个5 -(2)拮抗剂。体内氟立班丝氨结合同样5 - (1 a)和5 (2 a)受体。然而,在更高水平的大脑5 -(即。,在压力下),氟立班丝氨可能占据5 - (2 a)受体的比例高于5 - (1 a)受体。氟立班丝氨对腺苷酸环化酶的影响不同于丁螺环酮和8-OH-DPAT,另外两个传说中的5 - (1 a)受体受体激动剂。氟立班丝氨降低神经元活动率中缝背的细胞,海马和皮层CA1区是大脑中最敏感的。Flibanserin-induced降低燃烧速度似乎在皮层介导通过刺激突触后5 - (1 a)受体,而活性细胞的数量的减少似乎是通过刺激多巴胺D(4)受体介导的。氟立班丝氨迅速逐渐脱敏体细胞5 -受体在中缝背和增强滋补激活突触后5 - (1 a)受体在CA3区域。氟立班丝氨优先减少合成和细胞外水平的5 -皮层,它增强了细胞外的NE、DA水平。 Flibanserin displays antidepressant-like activity in most animal models sensitive to antidepressants. Such activity, however, seems qualitatively different from that exerted by other antidepressants. Flibanserin seems to act via direct or indirect stimulation of 5-HT(1A), DA, and opioid receptors in those animal models. Flibanserin does not display consistent effects in animal models of anxiety and seems to exert potential antipsychotic effects. Flibanserin may induce some sedation but does not induce observable toxic effects at pharmacologically relevant doses.