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Titolo:
KINETIC-ANALYSIS OF MUSCARINIC RECEPTORS IN HUMAN BRAIN AND SALIVARY-GLAND IN-VIVO
Autore:
HIRAMATSU Y; ECKELMAN WC; CARRASQUILLO JA; MILETICH RS; VALDEZ IH; KURRASCH RHM; MACYNSKI AA; PAIK CH; NEUMANN RD; BAUM BJ;
Indirizzi:
NIDR,DEPT NUCL MED,CLIN INVEST & PATIENT CARE BRANCH,BLDG 10,RM 1N113BETHESDA MD 20892 NIDR,DEPT NUCL MED,CLIN INVEST & PATIENT CARE BRANCH BETHESDA MD 20892 NIH,DEPT POSITRON EMISS TOMOG BETHESDA MD 20892
Titolo Testata:
American journal of physiology. Regulatory, integrative and comparative physiology
fascicolo: 6, volume: 37, anno: 1995,
pagine: 1491 - 1499
SICI:
0363-6119(1995)37:6<1491:KOMRIH>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; ACETYLCHOLINE-RECEPTORS; INACTIVE ENANTIOMERS; RAT-BRAIN; INVIVO; BINDING; QUANTIFICATION; CYCLOFOXY; TRANSPORT; SUBTYPES;
Keywords:
QUINUCLIDINYL IODOBENZILATE; PHARMACOKINETICS; MUSCARINIC-CHOLINERGIC RECEPTORS; HUMAN STUDIES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
30
Recensione:
Indirizzi per estratti:
Citazione:
Y. Hiramatsu et al., "KINETIC-ANALYSIS OF MUSCARINIC RECEPTORS IN HUMAN BRAIN AND SALIVARY-GLAND IN-VIVO", American journal of physiology. Regulatory, integrative and comparative physiology, 37(6), 1995, pp. 1491-1499

Abstract

Previous studies in rats have suggested that the muscarinic acetylcholine receptor (mAChR) antagonist (S)-3-quinuclidinyl-(S)-4-[I-123]iodobenzilate [(SS)-IQNB] may be useful for the in vivo evaluation of mAChRs in humans as a control for the higher-affinity compound (RR)-IQNB. We have directly tested this hypothesis and examined the distribution of mAChRs in brain regions and parotid glands of healthy human volunteers in vivo using (RR)- and (SS)-IQNB (relatively high- and low-affinity antagonists, respectively), planar imaging, and pharmacokinetic analysis. This is the first in vivo study of mAChRs in humans that has employed stereoisomeric ligands and metabolic analysis to determine specific receptor binding. We observed that (SS)-IQNB showed much faster clearance from blood than (RR)-IQNB and different metabolite profiles. Also, the transport kinetics of the enantiomers were different. The estimated binding potential (similar to B-max/K-d) of (RR)-IQNB was highest in two cortical regions, intermediate in parotid gland, and lowestin cerebellum. The aggregate results show that in humans (SS)-IQNB does not act as an ideal general probe to measure the nonspecific IQNB distribution. However, (RR-) IQNB does appear to have value when used for studies of human brain mAChRs.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/09/20 alle ore 03:09:47