Constanti A
J Physiol (Paris). 1979;75(6):645-9.
A quantitative study was made of the action of GABA, some structurally-related agonists and antagonists on the dactyl opener muscle fibres of the lobster. It was concluded that the GABA dose/conductance relationship was better described by a two independent binding-site receptor model (with KII = 30 microM) than by a single-site or a two-site high co-operativity model. The dose/conductance curves for gamma-amino-beta-hydroxybutyric acid (GABOB), delta-aminovaleric acid (DAV) and piperazine indicated 'full' agonist behaviour, whereas those for guanidoacetic acid (GuAc) indicated a partial agonist action. beta-guanidinopropionic acid (beta-GP) and gamma-guanidinobutyric acid (gamma-GB) behaved as weak competitive GABA antagonists. Bicuculline was found to antagonize GABA non-competitively on the lobster as in the crayfish, whereas picrotoxin appeared to act in a 'mixed' antagonistic fashion.
对γ-氨基丁酸（GABA）、一些结构相关的激动剂和拮抗剂对龙虾开指肌纤维的作用进行了定量研究。得出的结论是，与单位点或双位点高协同性模型相比，双独立结合位点受体模型（KII = 30微摩尔）能更好地描述GABA剂量/电导关系。γ-氨基-β-羟基丁酸（GABOB）、δ-氨基戊酸（DAV）和哌嗪的剂量/电导曲线表明其具有“完全”激动剂行为，而胍基乙酸（GuAc）的剂量/电导曲线表明其具有部分激动剂作用。β-胍基丙酸（β-GP）和γ-胍基丁酸（γ-GB）表现为弱竞争性GABA拮抗剂。发现荷包牡丹碱在龙虾中与在小龙虾中一样对GABA具有非竞争性拮抗作用，而印防己毒素似乎以“混合”拮抗方式起作用。
