Tan S, Curtis-Prior P B
Pharmacol Res Commun. 1984 May;16(5):461-6. doi: 10.1016/s0031-6989(84)80014-4.
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.
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。