Abstract
Some pharmacological actions of (±) — cis — and (±) — trans -2-(aminomethyl) cyclopropane carboxylic acids, conformationally restricted analogues of GABA, are described. The trans isomer (TAMP) was 17 and 4.5 times less active than GABA in hyperpolarising central neurones of Limulus and Periplanata and 10.8 times less active in displacing [ 3H]-muscimol from rat brain membranes. The cis isomer (CAMP) was ineffective on Limulusneurones at 35 μmoles, 650 times less active on Periplanata neurones and only weakly displaced [ 3H]-muscimol at 100 μm. Neither isomer inhibited synaptosomal uptake of [ 3H]-GABA at 100 μM. These data suggest that the invertebrate receptors studied respond to GABA in an extended conformation.
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