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Titolo:
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor
Autore:
Roth, BL; Ernsberger, P; Steinberg, S; Rao, S; Rauser, L; Savage, J; Hufeisen, S; Berridge, MS; Muzic, RF;
Indirizzi:
Case Western Reserve Univ, Sch Med, Dept Biochem, Cleveland, OH 44106 USA Case Western Reserve Univ Cleveland OH USA 44106 Cleveland, OH 44106 USA Case Western Reserve Univ, NIMH, Psychoact Drug Screening Program, Dept Biochem Psychiat & Neurosci,Sch Med, Cleveland, OH 44106 USA Case Western Reserve Univ Cleveland OH USA 44106 Cleveland, OH 44106 USA Case Western Reserve Univ, Sch Med, Dept Nutr, Cleveland, OH 44106 USA Case Western Reserve Univ Cleveland OH USA 44106 Cleveland, OH 44106 USA Univ Hosp Cleveland, Dept Radiol & Chem, Cleveland, OH 44106 USA Univ HospCleveland Cleveland OH USA 44106 Chem, Cleveland, OH 44106 USA Univ Hosp Cleveland, Dept Radiol & Biomed Engn, Cleveland, OH 44106 USA Univ Hosp Cleveland Cleveland OH USA 44106 Engn, Cleveland, OH 44106 USA
Titolo Testata:
PSYCHOPHARMACOLOGY
fascicolo: 1, volume: 157, anno: 2001,
pagine: 111 - 114
Fonte:
ISI
Lingua:
ENG
Soggetto:
MEMORY STORAGE; HUMAN-BRAIN; INVOLVEMENT; BINDING; AMYGDALA; STRESS;
Keywords:
positron emission tomography; beta-adrenergic; 5-HT1A;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
14
Recensione:
Indirizzi per estratti:
Indirizzo: Roth, BL Case Western Reserve Univ, Sch Med, Dept Biochem, Rm W438,10900 Euclid Ave, Cleveland, OH 44106 USA Case Western Reserve Univ Rm W438,10900 Euclid Ave Cleveland OH USA 44106
Citazione:
B.L. Roth et al., "The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor", PSYCHOPHAR, 157(1), 2001, pp. 111-114

Abstract

Rationale: s-Fluorocarazolol [(S)-FCZ] is the major positron emission tomography (PET) ligand currently used to visualize central P-adrenergic receptors in vivo, although its pharmacology is incompletely known. Objective: Our objective was to comprehensively characterize the in vitro pharmacology of (S)- and (R)-FCZ to determine its suitability for study of central and peripheral P-]l.beta -adrenergic receptors. Methods: We characterized the in vitro pharmacology of (S)-FCZ at 42 biogenic amine receptors and transporters in vitro using the resources of the National Institute of Mental Health Psychoactive Drug Screening Program. Results: As expected (R)- and (S)-FCZ had high affinities for beta -adrenergic receptors (Ki values=0.08-0.45 nM)and negligible affinities (Ki values > 100 nM) for nearly all other testedreceptors and transporters with the exception of the h5-HT1A receptor for which (S)-FCZ had high affinity (Ki=34 nM). Interestingly, (R)-FCZ had low affinity for the h5-HT1A receptor (Ki=342 nM). Conclusion: The high affinity of (S)-FCZ for the h5-HT1A receptor is not likely to interfere with studies of peripheral beta -adrenergic receptors, since 5-HT1A receptors are expressed at very low levels outside the central nervous system. Indeed, computer simulations predict that even at low ligand concentrations, 5-HT1A binding in brain regions like hippocampus are likely to be substantial. Thus, (S)-FCZ may not be a suitable PET ligand for studies of central nervous system beta -adrenergic receptors unless the contribution by 5-HT1A sites can be shown to be negligible.

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Documento generato il 19/09/20 alle ore 14:10:23