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Titolo:
Binding profiles of a series of 2-arylpropionic acid esters on cloned human muscarinic receptor subtypes (m(1)-m(5)) and their relationship to nootropic activity
Autore:
Ghelardini, C; Mizuma, I; Gualtieri, F; Bartolini, A; Galeotti, N; Romanelli, MN; Teodori, E;
Indirizzi:
Univ Florence, Dept Preclin & Clin Pharmacol, I-50134 Florence, Italy UnivFlorence Florence Italy I-50134 Pharmacol, I-50134 Florence, Italy Kyushu Univ, Dept Neuropharmacol, Fukuoka 812, Japan Kyushu Univ FukuokaJapan 812 v, Dept Neuropharmacol, Fukuoka 812, Japan Univ Florence, Dept Pharmaceut Sci, Florence, Italy Univ Florence Florence Italy ence, Dept Pharmaceut Sci, Florence, Italy
Titolo Testata:
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
fascicolo: 6, volume: 49, anno: 1999,
pagine: 483 - 488
SICI:
0004-4172(199906)49:6<483:BPOASO>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
PRESYNAPTIC CHOLINERGIC MODULATORS; POTENT COGNITION ENHANCERS; ANALGESIC DRUGS; ENANTIOMERS;
Keywords:
2-arylpropionic acid esters, effect on amnesia, effect on learning and memory, muscarinic binding profile; cholinergic system; muscarinic receptors;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Ghelardini, C Univ Florence, Dept Preclin & Clin Pharmacol, Viale Morgagni65, I-50134 Florence, Italy Univ Florence Viale Morgagni 65 Florence Italy I-50134 taly
Citazione:
C. Ghelardini et al., "Binding profiles of a series of 2-arylpropionic acid esters on cloned human muscarinic receptor subtypes (m(1)-m(5)) and their relationship to nootropic activity", ARZNEI-FOR, 49(6), 1999, pp. 483-488

Abstract

The muscarinic binding profile of a series of 2-arylpropionic acid esters on cloned human muscarinic receptor subtypes (m(1)-m(5)) was determined to investigate whether there is a correlation between pharmacological activityand muscarinic receptor subtype selectivity. Among the tested compounds, 1, 7 and 9 showed the highest affinity for them and m(4) receptors. Compounds 1, 7 and 9 show good affinity for m4 receptors (pKi = 7.87; 7.73 and 7.10, respectively) and are able to discriminate 10-60 fold between m(4)/m(1), m(4)/m(3), and m(4)/m(5) subtypes. Conversely, these compounds are able only to weakly discriminate between m(4)/m(2) Compounds 1 (50-300 mu g kg(-1) i.p.) and 7 (1-10 mu g kg(-1) i.p.), injected 20 min before the training session, are able to prevent the amnesia induced by dicyclomine (2 mg kg(-1) i.p.) in the mouse passive-avoidance test. Compounds 1 and 7, at the highest antiamnesic doses, do not modify motor coordination and spontaneous motility as evaluated by the rota-rod test and Animex apparatus experiments.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 15:22:54