Benfey B G, Yong M S, Belleau B, Melchiorre C
Can J Physiol Pharmacol. 1979 Jan;57(1):41-7. doi: 10.1139/y79-006.
Since many alpha-adrenoceptor blocking drugs were known to have muscarinic blocking activity, BHC, a newly synthesized tetramine disulfide with alpha-adrenoceptor blocking activity, and two of its analogs were tested for muscarinic blocking activity in the isolated guinea pig atrium and ileum. BHC had muscarinic blocking activity. Its potency was higher in the atrium than in the ileum. The cardiac muscarinic blocking potency of the analog that contained carbon atoms instead of sulfur atoms was similar to that of BHC. Lower concentrations of the drugs antagonized inotropic effects of acetylcholine competitively, but higher concentrations had a smaller effect than expected for competitive antagonism. In the atrium BHC competitively inhibited the muscarinic blocking effect of atropine. Its atropinic blocking potency was similar to the muscarinic blocking potency. Quinidine and gallamine also had muscarinic blocking and atropinic blocking effects in the atrium but were about 10 times less potent than BHC.
由于已知许多α-肾上腺素受体阻断药物具有毒蕈碱阻断活性，因此对一种新合成的具有α-肾上腺素受体阻断活性的四胺二硫化物BHC及其两种类似物在离体豚鼠心房和回肠中进行了毒蕈碱阻断活性测试。BHC具有毒蕈碱阻断活性。其在心房中的效力高于在回肠中的效力。含有碳原子而非硫原子的类似物的心脏毒蕈碱阻断效力与BHC相似。较低浓度的药物竞争性拮抗乙酰胆碱的变力作用，但较高浓度的药物作用比竞争性拮抗预期的要小。在心房中，BHC竞争性抑制阿托品的毒蕈碱阻断作用。其阿托品阻断效力与毒蕈碱阻断效力相似。奎尼丁和加拉明在心房中也有毒蕈碱阻断和阿托品阻断作用，但效力比BHC低约10倍。
