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RX 781094、米安色林、育亨宾、萝芙素和哌唑嗪对逆转可乐定抑制仓鼠分离白色脂肪细胞中促黑素刺激的脂肪分解的比较作用。

Comparative effects of RX 781094, mianserin, yohimbine, rauwolscine and prazosin in reversing clonidine inhibition of MIX-stimulated lipolysis in hamster isolated white fat cells.

作者信息

Tan S, Curtis-Prior P B

出版信息

Pharmacol Res Commun. 1984 May;16(5):461-6. doi: 10.1016/s0031-6989(84)80014-4.

Abstract

Different alpha-adrenergic receptor antagonists: RX 781094, yohimbine and rauwolscine (selective alpha 2-adrenergic antagonists); mianserin (tetracyclic anti-depressant, antagonist at alpha 2-presynaptic autoreceptors) and prazosin (selective alpha 1-adrenergic antagonist) were used at concentrations ranging from 10(-7) to 10(-4) M, to reverse clonidine inhibition of MIX-stimulated lipolysis in the hamster fat cell. In this adipose tissue (like human but unlike rat) there co-exist prolipolytic beta-adrenoceptors and antilipolytic alpha-adrenoceptors. Although no effects were observed with prazosin, RX 781094 was ten times more potent than yohimbine or its isomer rauwolscine in reversing clonidine inhibition of the MIX-stimulated lipolysis. Mianserin was an effective blocker only from a concentration of 10(-4) M, consistent with its relative lack of specificity for alpha 2-adrenoceptors cited elsewhere. Overall these results confirm the utility of this model for testing compounds presumed to act at alpha 2-adrenoceptors.

摘要

不同的α-肾上腺素能受体拮抗剂:RX 781094、育亨宾和萝芙素(选择性α2-肾上腺素能拮抗剂);米安色林(四环类抗抑郁药,α2-突触前自身受体拮抗剂)和哌唑嗪(选择性α1-肾上腺素能拮抗剂),使用浓度范围为10^(-7)至10^(-4) M,以逆转可乐定对仓鼠脂肪细胞中MIX刺激的脂解作用的抑制。在这种脂肪组织中(与人类相似但与大鼠不同),同时存在促脂解的β-肾上腺素能受体和抗脂解的α-肾上腺素能受体。虽然哌唑嗪未观察到作用,但在逆转可乐定对MIX刺激的脂解作用的抑制方面,RX 781094的效力比育亨宾或其异构体萝芙素强十倍。米安色林仅从10^(-4) M的浓度起才是有效的阻断剂,这与其在其他地方提到的对α2-肾上腺素能受体相对缺乏特异性一致。总体而言,这些结果证实了该模型在测试假定作用于α2-肾上腺素能受体的化合物方面的实用性。

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