Patel N B, Jindal M N, Patel V K
Arzneimittelforschung. 1978;28(7):1071-5.
20 newly synthesized glutarimide compounds and their organic bases were investigated for their action on the autonomic ganglion in cats. Compounds 1 to 7 having piperidine moiety showed mainly ganglionic stimulant activity as evidenced by rise in blood pressure, contraction of nictitating membrane and rise in urinary bladder pressure of cats, which was completely blocked by C6 and partly by atropine. Compound 8 and 9 having diethylamine moiety showed initial stimulation--followed by blockade of the autonomic ganglia. Compounds 10 to 13 having morpholine moiety showed stimulation of both sympathetic and parasympathetic autonomic nervous system. The responses were due to effect partly on ganglia and partly on the receptors. Compounds 14 to 20, which have alkyl substitution chain at position 4 of beta-carbon atom, showed depressor action. The ganglionic activity of the glutarimide compounds in various groups was found to be in inverse ratio to the length of the alkyl side chain at position 4 of the beta-carbon atom.
对20种新合成的戊二酰亚胺化合物及其有机碱对猫自主神经节的作用进行了研究。具有哌啶部分的化合物1至7主要表现出神经节兴奋活性，猫的血压升高、瞬膜收缩和膀胱压力升高证明了这一点，C6可完全阻断这种作用，阿托品可部分阻断。具有二乙胺部分的化合物8和9表现出初始兴奋，随后是自主神经节的阻断。具有吗啉部分的化合物10至13表现出对交感和副交感自主神经系统的刺激作用。这些反应部分是由于对神经节的作用，部分是由于对受体的作用。在β-碳原子的4位具有烷基取代链的化合物14至20表现出降压作用。发现戊二酰亚胺化合物在各个组中的神经节活性与β-碳原子4位烷基侧链的长度成反比。
