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Titolo:
Measurement of plasma metabolites of (S)-5-[I-123]iodo-3-(2-azetidinylmethoxy)pyridine (5-IA-85380), a nicotinic acetylcholine receptor imaging agent, in nonhuman primates
Autore:
Zoghbi, SS; Tamagnan, G; Fujita, M; Baldwin, RM; Al-Tikriti, MS; Amici, L; Seibyl, JP; Innis, RB;
Indirizzi:
Yale Univ, Sch Med, Dept Diagnost Radiol, New Haven, CT 06520 USA Yale Univ New Haven CT USA 06520 Diagnost Radiol, New Haven, CT 06520 USA Yale Univ, Sch Med, Dept Psychiat, New Haven, CT 06520 USA Yale Univ New Haven CT USA 06520 , Dept Psychiat, New Haven, CT 06520 USA Vet Adm Med Ctr, W Haven, CT 06516 USA Vet Adm Med Ctr W Haven CT USA 06516 t Adm Med Ctr, W Haven, CT 06516 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 1, volume: 28, anno: 2001,
pagine: 91 - 96
SICI:
0969-8051(200101)28:1<91:MOPMO(>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
CEREBRAL-CORTEX; SPECT; IOMAZENIL; BINDING;
Keywords:
in vivo metabolism; pharmacokinetics; nicotinic acetylcholine receptor; 5-IA-85380; [I-123]-5-IA-85380; (S)-5-[I-123]iodo-3-(2-azetidinylmethoxy)pyridine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
11
Recensione:
Indirizzi per estratti:
Indirizzo: Zoghbi, SS Yale Univ, Sch Med, Dept Diagnost Radiol, POB 208042,333 Cedar St, New Haven, CT 06520 USA Yale Univ POB 208042,333 Cedar St New Haven CT USA 06520 20 USA
Citazione:
S.S. Zoghbi et al., "Measurement of plasma metabolites of (S)-5-[I-123]iodo-3-(2-azetidinylmethoxy)pyridine (5-IA-85380), a nicotinic acetylcholine receptor imaging agent, in nonhuman primates", NUCL MED BI, 28(1), 2001, pp. 91-96

Abstract

The iodinated analog (S)-5-[I-123]iodo-3-(2-azetidinylmethoxy) of A-85380 is a new potential SPECT tracer specific for the alpha4 beta2 subtype nicotinic acetylcholine receptors, which play an important role in neurodegenerative diseases and in tobacco dependence. To evaluate the possibility of using this tracer for the in vivo quantification of these receptors, an accurate measurement of the plasma concentration of the parent compound is necessary. In human or nonhuman primate whole blood as well as in plasma, the parent compound is only stable for approximately 5 min, after which it decomposes. The radioligand is stable in the injection solution and in protein-free (>30 K M.W.) plasma ultrafiltrate for at least 18 h. To preserve the parent compound in plasma the radioactive plasma must be mixed with equal volumes of acetonitrile within 5 min after its collection or, alternatively, radioactive blood should be collected and mixed with sodium azide (3 mg/ml blood). The in vivo metabolism of [I-123]5-IA resulted in two components: a radiometabolite that is less lipophilic than the parent compound and a polar radiometabolite that is not free radioiodide because of the absence of radioactivity accumulation in the thyroid. (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/06/19 alle ore 17:33:30