Evans R H, Francis A A, Hunt K, Martin M R, Watkins J C
J Pharm Pharmacol. 1978 Jun;30(6):364-7. doi: 10.1111/j.2042-7158.1978.tb13257.x.
A new substnace, quisqualamine, the decarboxylated analogue of quisqualic acid, predictably depressed electrical activity of neurons of the frog and rat spinal cord in vitro and of the mouse spinal cord in vivo. In the in vitro preparations, the action of quisqualamine was associated with a prolonged depolarization of primary afferent terminals which was sensitive to blockade by picrotoxin and bicuculline and which was also depressed by strychnine. This suggests an interaction of quisqualamine with presynaptic receptors for both GABA and beta-alanine. Post-synaptic actions of quisqualamine, which were less marked than those at presynaptic sites, also appeared to be predominantly GABA-mimetic in vitro, though a sensitivity to the GABA-antagonist bicuculline could not be demonstrated in vitro.
一种新物质——喹唑啉胺,即喹唑啉酸的脱羧类似物,不出所料地抑制了青蛙和大鼠脊髓神经元在体外以及小鼠脊髓在体内的电活动。在体外实验制剂中,喹唑啉胺的作用与初级传入终末的去极化延长有关,这种去极化对苦味毒和荷包牡丹碱的阻断敏感,并且也会被士的宁抑制。这表明喹唑啉胺与γ-氨基丁酸(GABA)和β-丙氨酸的突触前受体存在相互作用。喹唑啉胺的突触后作用不如其在突触前部位的作用明显,在体外似乎也主要是模拟GABA的作用,尽管在体外无法证明其对GABA拮抗剂荷包牡丹碱敏感。