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Titolo:
Synthesis, analgesic activity, and binding properties of some epibatidine analogs with a tropine skeleton
Autore:
Radl, S; Hafner, W; Budesinsky, M; Hejnova, L; Krejci, I;
Indirizzi:
Res Inst Pharm & Biochem, CR-13060 Prague, Czech Republic Res Inst Pharm &Biochem Prague Czech Republic CR-13060 , Czech Republic Acad Sci Czech Republ, Inst Organ Chem & Biochem, CR-16610 Prague, Czech Republic Acad Sci Czech Republ Prague Czech Republic CR-16610 gue, Czech Republic
Titolo Testata:
ARCHIV DER PHARMAZIE
fascicolo: 6, volume: 333, anno: 2000,
pagine: 167 - 174
SICI:
0365-6233(200006)333:6<167:SAAABP>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
NICOTINIC ACETYLCHOLINE-RECEPTORS; SELECTIVE MUSCARINIC AGONISTS; HIGHLY POTENT; ANPIRTOLINE; ANTINOCICEPTION; DERIVATIVES; IDENTIFICATION; ABT-594; RODENTS; 5-HT1A;
Keywords:
epibatidine analogs; pyridinyl piperidines; analgesic activity; serotonin receptor ligands; muscarine receptor ligands; nicotine receptor ligands;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Radl, S Res Inst Pharm & Biochem, Kourimska 17, CR-13060 Prague, Czech Republic Res Inst Pharm & Biochem Kourimska 17 Prague Czech Republic CR-13060
Citazione:
S. Radl et al., "Synthesis, analgesic activity, and binding properties of some epibatidine analogs with a tropine skeleton", ARCH PHARM, 333(6), 2000, pp. 167-174

Abstract

A series of epibatidine analogs and their positional isomers bearing an 8-azabicyclo[3.2.1]octane moiety is described. Also some of their simplified analogs bearing a 3-piperidine moiety are reported. Their receptor binding profiles (5-HT1A, 5-HT1B, M-1, M-2, neuronal nicotinic receptor) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Some of the compounds, especially those containing an 8-azabicyclo[3.2.1]oct-2-ene moiety possess high afinity for the nicotinic cholinergic receptor. The most analgesically active compounds are also highly toxic. Optimized structures (PM3-MOPAC, Alchemy 2000, Tripos Inc.) of compounds 1-9 were compared with that of epibatidine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 00:29:13