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Titolo:
Synthesis and pharmacological evaluation of imidazoline sites I-1 and I-2 selective ligands
Autore:
Anastassiadou, M; Danoun, S; Crane, L; Baziard-Mouysset, G; Payard, M; Caignard, DH; Rettori, MC; Renard, P;
Indirizzi:
Univ Toulouse 3, Fac Pharm, Lab Chim Pharmaceut, F-31062 Toulouse 4, France Univ Toulouse 3 Toulouse France 4 Pharmaceut, F-31062 Toulouse 4, France Soc ADIR, F-92415 Courbevoie, France Soc ADIR Courbevoie France F-92415Soc ADIR, F-92415 Courbevoie, France
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 3, volume: 9, anno: 2001,
pagine: 585 - 592
SICI:
0968-0896(200103)9:3<585:SAPEOI>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
ALPHA-ADRENORECEPTOR REAGENTS; ADRENAL-MEDULLARY MEMBRANES; BINDING-SITES; VENTROLATERAL MEDULLA; PREFERRING RECEPTORS; I1-IMIDAZOLINE SITES; H-3 CLONIDINE; HIGH-AFFINITY; IDAZOXAN; ALPHA-2-ADRENOCEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
69
Recensione:
Indirizzi per estratti:
Indirizzo: Anastassiadou, M Univ Toulouse 3, Fac Pharm, Lab Chim Pharmaceut, 35 Chemin Maraichers, F-31062 Toulouse 4, France Univ Toulouse 3 35 Chemin Maraichers Toulouse France 4 e
Citazione:
M. Anastassiadou et al., "Synthesis and pharmacological evaluation of imidazoline sites I-1 and I-2 selective ligands", BIO MED CH, 9(3), 2001, pp. 585-592

Abstract

Several series of 2-aryl or heterocyclic-imidazoline compounds have been prepared and evaluated in vitro as imidazoline sites (I-1 and I-2) and alpha-adrenergic (alpha (1) and alpha (2)) receptor ligands. Their pK(i) valuesindicate that linkage of the imidazoline moiety at the 2-position with an aromatic substituent dramatically decreases alpha -adrenergic affinity. I-1sites are more accessible by phenyl imidazolines substituted by a methyl or a methoxy group at the ortho or meta position. Indeed, 2-(2'-methoxyphenyl)-imidazoline (17) is one of the best I-1 ligands ever reported (pK(i) = 8.53 and I-1/I-2 > 3388). On the other hand, I-2 selectivity increases in the presence of a methyl group in the para position. The original compound, 2-(3'-fluoro-4'-tolyl)-imidazoline (31) is a new potent ligand for the I-2 sites with high selectivity (pK(i) = 8.53 and I-2/I-1 > 3388). (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/20 alle ore 12:13:00