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Isoguvacine,isonipecotic acid,muscimol and N-methyl isoguvacine on the GABA receptor in rat sympathetic ganglia
Authors:N. G. Bowery  J. F. Collins  A. L. Hudson  M. J. Neal
Affiliation:(1) Departments of Pharmacology, St. Thomas's Hospital Medical School, SE1 7EH London, (England);(2) School of Pharmacy, 29/39 Brunswick Square, WC1N 1AX London, (England);(3) Department of Chemistry, City of London Polytechnic, 31 Jewry Street, EC3 London, (England)
Abstract:
Summary The GABA-mimetic activities of 4 analogues muscimol, isonipecotic acid, isoguvacine and N-methyl isoguvacine have been examined at the GABA receptor in the rat isolated superior cervical ganglion. The depolarizing action of all 4 analogues could be selectively antagonized by bicuculline methochloride and isopropyl bicyclophosphate. Muscimol was the only analogue more potent than GABA (molar potency ratio=5.08±0.707). The potency of isoguvacine was 0.23±0.026 and isonipecotic acid 0.011±0.0028. N.-methyl isoguvacine was <0.001 GABA.
Keywords:
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