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Titolo:
KINETIC-ANALYSIS OF RAT EXOCRINE GLAND MUSCARINIC RECEPTORS IN-VIVO
Autore:
HIRAMATSU Y; KAWAI R; REBA RC; BLASBERG RG; BAUM BJ;
Indirizzi:
NIDR,CLIN INVEST & PATIENT CARE BRANCH,BLDG 10,ROOM 1N-113 BETHESDA MD 20892 NIDR,CLIN INVEST & PATIENT CARE BRANCH BETHESDA MD 20892 NIH,CTR CLIN,DEPT NUCL MED BETHESDA MD 20892 UNIV CHICAGO,DEPT RADIOL CHICAGO IL 60637 MEM SLOAN KETTERING CANC CTR,DEPT NEUROONCOL NEW YORK NY 10021
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 269, anno: 1994,
pagine: 1205 - 1212
SICI:
0022-3565(1994)269:3<1205:KOREGM>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; ACETYLCHOLINE-RECEPTORS; BINDING-SITES; BLOOD-FLOW; INVIVO; BRAIN; ANTAGONISTS; TRANSPORT; MEMBRANES; AFFINITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
Y. Hiramatsu et al., "KINETIC-ANALYSIS OF RAT EXOCRINE GLAND MUSCARINIC RECEPTORS IN-VIVO", The Journal of pharmacology and experimental therapeutics, 269(3), 1994, pp. 1205-1212

Abstract

Recently we employed two enantiomers of the muscarinic antagonist quinuclidinyl iodobenzilate (IQNB), and pharmacokinetic analyses, to define and quantitate nonspecific and specific binding to rat parotid gland muscarinic acetylcholine receptors (mAChRs) in vivo (Hiramatsu et al., 1993). The present studies were designed to utilize this same approach for evaluating mAChRs in three other morphologically different ratexocrine glands: the submandibular, sublingual and lacrimal glands. The metabolism and tissue distribution of the intravenously injected IQNB enantiomers were determined, and the resulting data were assessed in terms of their goodness of fit to several multicompartmental models. All three exocrine glands showed substantial nonspecific ligand distribution as measured with the receptor-inert enantiomer (SS)-IQNB. Nonspecific distribution represented 45, 21 and 36% of total ligand distribution in submandibular, sublingual and lacrimal glands, respectively,as measured with the receptor-active enantiomer (RR)-IQNB. The rank order of the binding potential, kinetically equivalent to B-max/K-d, for(RR)-IQNB and these mAChRs was lacrimal > sublingual > submandibular glands (674 +/- 235 > 575 +/- 109 > 345 +/- 29). These results demonstrate that specific mAChRs in the exocrine glands can be measured in vivo with the (RR)-IQNB enantiomer and that despite some small quantitative differences, the distribution of (RR)- and (SS)-IQNB is similar inthe three exocrine glands but is substantially different from that inbrain and heart.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/11/20 alle ore 22:39:11