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首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Differential effects of centrally-active antihypertensives on 5-HT1A receptors in rat dorso-lateral septum rat hippocampus and guinea-pig hippocampus.
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Differential effects of centrally-active antihypertensives on 5-HT1A receptors in rat dorso-lateral septum rat hippocampus and guinea-pig hippocampus.

机译：中枢性降压药对大鼠背外侧隔大鼠海马和豚鼠海马中5-HT1A受体的差异作用。

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1. The electrophysiological responses elicited by 5-hydroxytryptamine1A-(5-HT1A) receptor agonists in rat and guinea-pig CA1 pyramidal neurones and rat dorso-lateral septal neurones were compared in vitro by use of conventional intracellular recording techniques. 2. In the presence of 1 microM tetrodotoxin (TTX), to prevent indirect effects, 5-HT, N,N-dipropyl-5-carboxamidotryptamine (DP-5-CT) and 8-hydroxy-2(di-n-propylamino) tetralin (8-OH-DPAT) hyperpolarized the neurones from rat and guinea-pig brain. 3. The hypotensive drug flesinoxan, a selective 5-HT1A receptor agonist, hyperpolarized neurones in all three areas tested; however, another hypotensive agent with high affinity at 5-HT1A-receptors, 5-methyl-urapidil, hyperpolarized only the neurones in rat hippocampus and septum. 4. In guinea-pig hippocampal neurones, 5-methyl-urapidil behaved as a 5-HT1A-receptor antagonist. 5. The relative efficacies (5-HT = 1) of DP-5-CT, 8-OH-DPAT, flesinoxan and 5-methyl-urapidil at the three sites were: rat hippocampus, 1.09, 0.7, 0.5 and 0.24; rat septum, 0.88, 0.69, 0.82 and 0.7; guinea-pig hippocampus, 1.0, 0.69, 0.89 and 0, respectively. 6. It is concluded that the hypotensive agents flesinoxan and 5-methyl-urapidil appear to have different efficacies at 5-HT1A receptors located in different regions of the rodent brain. Whether these regional and species differences arise from receptor plurality or variability in intracellular transduction mechanisms remains to be elucidated.
机译：1.通过使用常规细胞内记录技术，比较了5-羟基色胺1A-（5-HT1A）受体激动剂在大鼠和豚鼠CA1锥体神经元和大鼠背外侧中隔神经元中引起的电生理反应。 2.为了防止间接作用，在存在1 microM河豚毒素（TTX）的情况下，使用5-HT，N，N-二丙基-5-羧酰胺基色胺（DP-5-CT）和8-羟基-2（二正丙基氨基）四氢萘（8-OH-DPAT）使大鼠和豚鼠大脑的神经元超极化。 3.在所有三个测试领域中，降压药“ fesinoxan”（一种选择性的5-HT1A受体激动剂）均具有超极化神经元。然而，另一种对5-HT1A受体具有高亲和力的降压药5-甲基-乌拉地尔只使大鼠海马和隔膜的神经元超极化。 4.在豚鼠海马神经元中，5-甲基-乌拉地尔起5-HT1A受体拮抗剂的作用。 5. DP-5-CT，8-OH-DPAT，氟苯恶烷和5-甲基-尿嘧啶在这三个部位的相对效率（5-HT = 1）为：大鼠海马，1.09、0.7、0.5和0.24；大鼠中隔，0.88，0.69，0.82和0.7;豚鼠海马分别为1.0、0.69、0.89和0。 6.结论是，降压药flesinoxan和5-甲基-尿嘧啶对位于啮齿动物大脑不同区域的5-HT1A受体似乎具有不同的功效。这些区域和物种差异是由于受体的多样性还是细胞内转导机制的变异性引起的，尚待阐明。

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