The activity of cis and trans -2- (aminomethyl) cyclopropane carboxylic acids on gaba — related mechanisms in the central nervous system of limulus and periplanata and of mammals
| Autor: | L. Chidley, S. Clements-Jewery, C.J. Roberts, Robert J. Walker, C.R. Gardner |
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| Rok vydání: | 1982 |
| Předmět: |
Central Nervous System
Cyclopropanes Stereochemistry Central nervous system Molecular Conformation Cockroaches In Vitro Techniques Binding Competitive Cyclopropane Cellular and Molecular Neuroscience chemistry.chemical_compound Species Specificity Horseshoe Crabs medicine Animals Receptor gamma-Aminobutyric Acid Neurons Pharmacology biology Muscimol biology.organism_classification Rat brain Rats Membrane medicine.anatomical_structure nervous system chemistry Limulus Cis–trans isomerism Synaptosomes |
| Zdroj: | Neuropharmacology. 21:197-200 |
| ISSN: | 0028-3908 |
| Popis: | 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 [ 3 H]-muscimol from rat brain membranes. The cis isomer (CAMP) was ineffective on Limulus neurones at 35 μmoles, 650 times less active on Periplanata neurones and only weakly displaced [ 3 H]-muscimol at 100 μm. Neither isomer inhibited synaptosomal uptake of [ 3 H]-GABA at 100 μM. These data suggest that the invertebrate receptors studied respond to GABA in an extended conformation. |
| Databáze: | OpenAIRE |
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