Harvey A L, Paul D, Rodger I W, Singh H
J Pharm Pharmacol. 1976 Aug;28(8):617-9. doi: 10.1111/j.2042-7158.1976.tb02812.x.
The effects of the newly synthesized neuromuscular blocking agent, chandonium iodide (17a-methyl-3beta-pyrrolidino-17a-aza-D-homo-5-androstene dimethiodide) have been investigated on guinea-pig isolated ileum and vas deferens preparations. On the ileum, chandonium (0-1-10-0 mug ml(-1); 1-6 X 10(-7) M-1-6 X 10(-5) M) had weak muscarinic receptor blocking action (pA2 is 5-7), but no antihistamine properties at the concentration tested. No evidence for anticholinesterase actions was found. On the vas deferens, chandonium (10-50 mug ml(-1); 1-6-8-1 X 10(-5) M) potentiated responses to exogenous noradrenaline; responses to electrical stimulation were potentiated only in the presence of 50 mug ml(-1) chandonium. No adrenoceptor or adrenergic neuron blockade was found. The results provide evidence that chandonium acts selectively at acetylcholine receptors and that it is more active as a nicotinic receptor antagonist than as a muscarinic receptor antagonist.
研究了新合成的神经肌肉阻滞剂碘化钱度（17a - 甲基 - 3β - 吡咯烷基 - 17a - 氮杂 - D - 高 - 5 - 雄烯二甲基碘化物）对豚鼠离体回肠和输精管标本的作用。在回肠上，钱度（0.1 - 10.0μg/ml；1.6×10⁻⁷M - 1.6×10⁻⁵M）具有较弱的毒蕈碱受体阻断作用（pA₂为5.7），但在所测试的浓度下无抗组胺特性。未发现抗胆碱酯酶作用的证据。在输精管上，钱度（10 - 50μg/ml；1.6 - 8.1×10⁻⁵M）增强了对外源性去甲肾上腺素的反应；仅在存在50μg/ml钱度时，对电刺激的反应增强。未发现肾上腺素能受体或肾上腺素能神经元阻断作用。结果表明，钱度选择性作用于乙酰胆碱受体，且作为烟碱受体拮抗剂比作为毒蕈碱受体拮抗剂更具活性。
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