中枢型苯二氮䓬受体在抑制促甲状腺激素释放激素诱导的大鼠垂体灌流液中促甲状腺激素释放方面作用的证据。
Evidence for a role of central type benzodiazepine receptors in the inhibition of the thyrotropin-releasing hormone-induced thyrotropin release from rat perifused pituitaries.
作者信息
Tapia-Arancibia L, Alonso R, Astier H
出版信息
Neurosci Lett. 1986 Nov 21;71(3):329-34. doi: 10.1016/0304-3940(86)90642-7.
Several centrally active benzodiazepines (BZ) were tested for their ability to inhibit the TRH-induced secretion of TSH in vitro from perifused pituitaries. Diazepam, flurazepam, chlordiazepoxide (CDZ) and midazolam (10 nM) inhibited the TSH response to TRH (10 nM) by 33-50%, while medazepam, a prodrug having virtually no affinity for central BZ sites, did not. CDZ inhibition was reversed by Ro 15-1788, antagonist of the central type BZ binding sites, but not by PK 11195, antagonist of the peripheral type. The data are consistent with an involvement of central type BZ receptor sites in the TSH-lowering effects of BZ in rats.
对几种中枢活性苯二氮䓬类药物（BZ）进行了测试，以考察它们在体外抑制经灌流的垂体中促甲状腺激素释放激素（TRH）诱导的促甲状腺激素（TSH）分泌的能力。地西泮、氟西泮、氯氮䓬（CDZ）和咪达唑仑（10 nM）可使TSH对TRH（10 nM）的反应抑制33%-50%，而美达西泮，一种对中枢BZ位点几乎没有亲和力的前体药物，则无此作用。CDZ的抑制作用可被中枢型BZ结合位点拮抗剂Ro 15-1788逆转，但不能被外周型拮抗剂PK 11195逆转。这些数据表明，中枢型BZ受体位点参与了BZ对大鼠TSH降低的作用。
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