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Titolo:
SITES OF ACTION OF NONCOMPETITIVE GABA ANTAGONISTS IN HOUSEFLIES AND RATS - 3-DIMENSIONAL QSAR ANALYSIS
Autore:
AKAMATSU M; OZOE Y; UENO T; FUJITA T; MOCHIDA K; NAKAMURA T; MATSUMURA F;
Indirizzi:
KYOTO UNIV,DEPT AGR CHEM KYOTO 60601 JAPAN SHIMANE UNIV,DEPT LIFE SCI & BIOTECHNOL MATSUE SHIMANE 690 JAPAN UNIV CALIF DAVIS,DEPT ENVIRONM TOXICOL DAVIS CA 95616 UNIV CALIF DAVIS,DEPT ENTOMOL DAVIS CA 95616
Titolo Testata:
Pesticide science
fascicolo: 4, volume: 49, anno: 1997,
pagine: 319 - 332
SICI:
0031-613X(1997)49:4<319:SOAONG>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
GATED CHLORIDE CHANNEL; CYCLODIENE-TYPE INSECTICIDES; AMINOBUTYRIC-ACID RECEPTORS; PICROTOXININ RECEPTOR; GROUND-STATES; HIGH-AFFINITY; BINDING; BRAIN; ENDOSULFAN; PARAMETERS;
Keywords:
PICROTOXININ-TYPE GABA ANTAGONISTS; COMPARATIVE MOLECULAR FIELD ANALYSIS; COMFA; INSECTICIDAL ACTIVITY AGAINST HOUSEFLIES; COMPETITIVE ACTIVITY AGAINST SPECIFIC [S-35] TBPS BINDING TO RAT BRAIN MEMBRANES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
M. Akamatsu et al., "SITES OF ACTION OF NONCOMPETITIVE GABA ANTAGONISTS IN HOUSEFLIES AND RATS - 3-DIMENSIONAL QSAR ANALYSIS", Pesticide science, 49(4), 1997, pp. 319-332

Abstract

Quantitative structure-activity relationships for insecticidal activity (against houseflies) and competitive activity against a specific [S-35]tert-butyl-bicyclophosphorothionate binding (to rat brain membranes) of some picrotoxinin-type 4-aminobutyric acid antagonists, including gamma-BHC, endosulfan, bicyclophosphates, dioxatricyclododecenes andrelated compounds, were examined three-dimensionally using comparative molecular field analysis (CoMFA). The antagonists were classified into two series according to their molecular shapes: i.e. whether their structure was 'linearly' extended beyond the 'mast-head' position of the 'boat-like' skeletons (series 1) or not (series 2). The CoMFA showed that the slopes in steric and electrostatic fields around the molecule were significant for both series in governing the potency variations in insecticidal and binding activities. Hydrophobicity, a possible factor controlling transport behaviour of compounds, was significant ingoverning variations in insecticidal activity, but not for the case of the rat membrane binding. Assuming that there is a slight topological difference between series 1 and 2 compounds in terms of the mode of binding with the housefly receptor site, the insecticidal activity wasanalysable with a single equation for the combined set of compounds, but the rat membrane binding was not. The sterically and electrostatically favourable regions surrounding the molecular series indicated by CoMFA were roughly located at positions so as to interact with the binding subsites on the receptors proposed previously.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 11:15:24