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Titolo:
Measurement of alpha(4)beta(2) nicotinic acetylcholine receptors with [I-123]5-I-A-85380 SPECT
Autore:
Fujita, M; Tamagnan, G; Zoghbi, SS; Al-Tikriti, MS; Baldwin, RM; Seibyl, JP; Innis, RB;
Indirizzi:
VA Connecticut, W Haven, CT 06516 USA VA Connecticut W Haven CT USA 06516VA Connecticut, W Haven, CT 06516 USA Yale Univ, Sch Med, Dept Psychiat, W Haven, CT 06516 USA Yale Univ W Haven CT USA 06516 Med, Dept Psychiat, W Haven, CT 06516 USA Yale Univ, Sch Med, Dept Diagnost Radiol, W Haven, CT 06516 USA Yale UnivW Haven CT USA 06516 ept Diagnost Radiol, W Haven, CT 06516 USA Yale Univ, Sch Med, Dept Pharmacol, W Haven, CT 06516 USA Yale Univ W Haven CT USA 06516 Med, Dept Pharmacol, W Haven, CT 06516 USA
Titolo Testata:
JOURNAL OF NUCLEAR MEDICINE
fascicolo: 9, volume: 41, anno: 2000,
pagine: 1552 - 1560
SICI:
0161-5505(200009)41:9<1552:MOANAR>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUBUNIT MESSENGER-RNAS; CENTRAL NERVOUS-SYSTEM; IN-VIVO; BINDING-SITES; HUMAN-BRAIN; ALPHA-BUNGAROTOXIN; ALZHEIMERS-DISEASE; NONHUMAN-PRIMATES; H-3 NICOTINE; RAT-BRAIN;
Keywords:
nicotinic receptors; 3-[2(S)-2-azetidinylmethoxy]pyridine; SPECT; compartment analysis; equilibrium analysis;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
40
Recensione:
Indirizzi per estratti:
Indirizzo: Fujita, M VA Connecticut, 116A2,950 Campbell Ave, W Haven, CT 06516 USA VAConnecticut 116A2,950 Campbell Ave W Haven CT USA 06516 6 USA
Citazione:
M. Fujita et al., "Measurement of alpha(4)beta(2) nicotinic acetylcholine receptors with [I-123]5-I-A-85380 SPECT", J NUCL MED, 41(9), 2000, pp. 1552-1560

Abstract

Nicotinic acetylcholine receptors (nAChRs) play an important role in tobacco dependence and a potential therapeutic role in neuropsychiatric disorders such as Alzheimer's disease. [I-123]5-iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-I-A-85380) is a new SP ECT tracer that labels alpha(4)beta(2) nAChRs. The purpose of this study was to assess the usefulness of this tracer to measure regional nAChR binding in baboon brain using both a bolus/kinetic paradigm and also a bolus plus constant infusion/equilibrium paradigm. Methods: A pair of bolus/kinetic and bolus plus constant infusion/equilibriumstudies was performed in each of 3 isoflurane-anesthetized baboons. Bolus studies were performed by intravenous injection of 191-226 MBq [I-123]5-I-A-85380 and image acquisition for 289-367 min. The data were analyzed with 1- and 2-tissue compartment models. Bolus plus constant infusion/ equilibrium studies were performed by a bolus injection (74-132 MBq) followed by a 468- to 495-min infusion with a bolus/infusion ratio (B/I) of 4.8-5.0 h. The distribution volumes in the thalamus were measured in these 2 paradigms. Tostudy whether the cerebellum was appropriate as a receptor-poor region, displacement studies were done in 2 baboons using the B/I paradigm with subcutaneous injection of (-)-cytisine (0.8 and 1.0 mg/kg). Results: The kinetics of this tracer was best described by the 1-tissue compartment model. The 2-compartment model showed poor identifiability of rate constants. The total (specific plus nondisplaceable compartments) distribution volumes (VT') agreed between bo[us and B/I paradigms (average percentage difference in VT',16.8%). (-)-Cytisine (0.8 and 1.0 mg/kg) displaced 70% and 72% of the radioactivity in the thalamus and 36% and 55% in the cerebellum, respectively, indicating that the latter was not appropriate as a receptor-poor region. Conclusion: These results show the feasibility of quantifying alpha(4)beta(2) nAChRs using [I-123]5-I-A-85380 and support the use of V-T' as an appropriate outcome measure.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 17:05:56