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Titolo:
Effect of SR121463, a selective non-peptide vasopressin V-2 receptor antagonist, in a rabbit model of ocular hypertension
Autore:
Lacheretz, F; Barbier, A; Serradeil-Le Gal, C; Elena, PP; Maffrand, JP; Le Fur, G;
Indirizzi:
Sanofi Rech, Dept Toxicol & Gen Pharmacol, F-34184 Montpellier 04, France Sanofi Rech Montpellier France 04 rmacol, F-34184 Montpellier 04, France
Titolo Testata:
JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS
fascicolo: 3, volume: 16, anno: 2000,
pagine: 203 - 216
SICI:
1080-7683(200006)16:3<203:EOSASN>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
CARBONIC-ANHYDRASE INHIBITOR; ATRIAL-NATRIURETIC-PEPTIDE; OPEN-ANGLE GLAUCOMA; INTRAOCULAR-PRESSURE; ARGININE-VASOPRESSIN; ANESTHETIZED RATS; WATER CHANNEL; CYNOMOLGUS MONKEY; HUMAN EYES; PILOCARPINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
50
Recensione:
Indirizzi per estratti:
Indirizzo: Lacheretz, F Sanofi Rech, Dept Toxicol & Gen Pharmacol, Ave Pr Blayac, F-34184 Montpellier 04, France Sanofi Rech Ave Pr Blayac Montpellier France 04 r 04, France
Citazione:
F. Lacheretz et al., "Effect of SR121463, a selective non-peptide vasopressin V-2 receptor antagonist, in a rabbit model of ocular hypertension", J OCUL PH T, 16(3), 2000, pp. 203-216

Abstract

The activity on intraocular pressure (IOP) of SR121463, a selective non-peptide arginin-vasopressin (AVP) V-2 receptor antagonist, was investigated in a rabbit model of ocular hypertension. We first demonstrated that, in vitro, SR121463 displayed high competitive affinity for rabbit vasopressin V-2 receptors (Ki = 2.1 +/- 1.2 nM). In vivo, SR121463 was instilled once (at concentrations ranging from 0.1 to 3%), or for 10 days (20 instillations) at 1% concentration, in the eye ofocular hypertensive rabbits (intraocular injection of 0.14 mg alpha-chymotrypsin). SR121463 also was instilled at 1% in the normotensive eye or intravenously injected (100 mu g/kg) to ocular hypertensive rabbits. SR121463 was compared to timolol 0.5% or to clonidine 0.25%. Additionally, local and systemic safety aspects were examined. Results showed that SR121463 was locally well-tolerated and had no anesthetic effect. A significant decrease in IOP of the hypertensive eye was observed for concentrations of SR121463 greater than or equal to 1%. This decrease was comparable to that obtained with reference compounds. A similar activity was found after intravenous administration. No tachyphylaxis was observed after 10 days, and no contralateral or systemic effect was noted. Also,when applied on the normotensive eye or when intravenously injected, SR121463 had no effect on the normotensive eye. These results on IOP and the good local and systemic safety profile, suggest that a potent vasopressin V-2 receptor antagonist, SR121463, could be ofvalue for the treatment of glaucoma, through a mechanism of action that remains to be elucidated.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 12:46:51