Detail of "4033-39-0"

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The action of gamma-aminobutyric acid (GABA) and ethylenediamine (EDA) on Limulus and Helix central neurons and rat cerebellar and sympathetic ganglion neurons

The action of gamma-aminobutyric acid (GABA) and ethylenediamine (EDA) on Limulus and Helix central neurons and rat cerebellar and sympathetic ganglion neurons. Bokisch, Anita J.; Bold, Jane M.; Gardner, C. R.; Perkins, M. N.; Roberts, C. Jane; Stone, T. W.; Walker, R. J. (Sch. Biochem. Physiol. Sci., Univ. Southampton, Southampton SO9 3TU, UK). Gen. Pharmacol., 15(6), 497-504 (English) 1984. CODEN: GEPHDP. ISSN: 0306-3623. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Intracellular recordings were made from central Limulus and Helix neurons and extracellular recordings from rat cerebellar Purkinje cells (P) and cervical sympathetic ganglia (CSG). The actions of GABA [56-12-2] and EDA [107-15-3] and related analogs on these prepns. were investigated. On Limulus neurons inhibited by GABA, EDA and piperazine [110-85-0] were 81- and 186-fold, resp., less potent than GABA. Both the GABA and EDA events were Cl- mediated, having similar reversal potentials, and were reversibly antagonized by picrotoxin. The EDA response persisted in high-Mg2+ Ringer. On Helix neurons inhibited by GABA, EDA was 92-fold less potent, whereas on neurons excited by GABA, EDA was 9.25-fold less potent. The other analogs tested had little or no GABA-like effect on either prepn. On P, EDA was equipotent with GABA and both compds. were antagonized by bicuculline. Flurazepam [17617-23-1] only potentiated the action of EDA on 3 of 23 cells tested, whereas the GABA response of all 23 cells was potentiated by the benzodiazepine. 2, 3-Diaminopropionic acid [4033-39-0] was a weak inhibitor of P firing, but flurazepam potentiated this response in 6 of 10 cells tested. On rat CSG neurons, EDA had 1/2 the potency of GABA and likewise the other analogs were less potent than GABA as depolarizing agents. Incubation with glutamic acid decarboxylase inhibitors had no effect on the EDA response. Cross desensitization between GABA and EDA was demonstrated in the CSG. Thus, EDA acts directly to activate at least part of the GABA receptor although the benzodiazepine receptors do not appear to be directly linked to the EDA component of the GABA receptor.

Spasmogenic and potentiating actions of some amino acids on the guinea pig myometrium

Spasmogenic and potentiating actions of some amino acids on the guinea pig myometrium. Bedwani, J. R.; Ishizawa, M.; Pickles, V. R.; Suwankrughasn, Surang (Dep. Physiol., Univ. Coll., Cardiff, Wales). Br. J. Pharmacol., 61(2), 217-22 (English) 1977. CODEN: BJPCBM. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Interactions) Thirty-three amino acids were applied sep. (2-10mM) to guinea-pig uterine horns in vitro at pH 7.4; L-glycine [56-40-6] and the straight-chain L-a-amino acids up to L-norleucine [327-57-1] produced contractions but the D-isomers were less potent or inactive. The w-amino acids, GABA [56-12-2] and d-aminovaleric acid [660-88-8], and the a,w-diamino acids, L-a,b-diaminopropionic acid [4033-39-0] and a,g-diaminobutyric acid [1758-80-1], produced contractions but b-alanine [107-95-9] and L-lysine [56-87-1] did not. L-Glutamic acid [56-86-0] and DL-homocysteic acid [504-33-6] were more active than L-glutamine [56-85-9] and L-asparagine [70-47-3]; L-histidine [71-00-1] and L-phenylalanine [63-91-2] showed little or no activity. The responses to the amino acids were not mediated by histamine, 5-hydroxytryptamine, acetylcholine, noradrenaline, or prostaglandins. Some of the amino acids that were spasmogenic at 2 to 10mM transiently potentiated other spasmogens at subspasmogenic concns.; the potentiating effect was also shown by a mixt. of amino acids at normal plasma concns. There was some similarity between the spasmogenic activities of different amino acids and their abilities to depolarize neurons.