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РЖ ВИНИТИ 34 (BI36) 96.04-04А4.377

Sigma receptor mapping [Text] : abstr. Book 41th Annu. Meet., Orlando, Fla, June 5-8, 1994 / Y. -W. Jung [et al.] // J. Nucl. Med. - 1994. - Vol. 35, N 5 Suppl. - P93 . - ISSN 0161-5505
Перевод заглавия: Картирование сигма-рецепторов
Аннотация: Iodine-125 labeled (+)-7-IBVM (Sp. Act. = 105-170 Ci/mmol, log P=3,43) has a whole brain concentration in CD-l mice of 1.03% dose 4 h after i.v. injection. Regional tracer distribution is consistent with regional sigma receptor density: cerebellum cortex hippocampus striatum. Cerebellum-to-blood concentration ratio, the best index of in vivo sigma receptor (SR) binding, rises from 7 at 4 h to 32 at 24 h. Pretreatment with haloperidol (1 mg/kg, i.p.), a potent SR antagonist, decreases 4 h cerebellar uptake by 85%; similar decreases are seen in cortex and hippocampus. Ex vivo autoradiographic analysis in rats confirms the gross regional tracer distribution observed in mice; in addition, markedly high tracer concentration was observed in the Purkinje layers of the cerebellum, granular layers of the dentate gyrus, and cranial nerve nuclei. Analysis of (+)-7-IBVM SR binding in guinea pig brain membranes versus [H-3]DTG gave K[i]=0.32 nM; the enantiomer, (-)-7-IBVM, has K[1]=1.56 nM. In vitro binding to other receptor sites was low: vesamicol (20 nM), alpha[1] (112 nM), D[2]('мю'M). Despite the high potency of SR binding observed with both enantiomers in vitro, the (-)-isomer, which is only 5-fold less potent, clears much more rapidly from the mouse cerebellum in vivo than does (+)-isomer: 4 h post-tracer injection, the cerebellar concentrations are 0.24 and 2.11% dose/g, respectively

ГРНТИ	34.49.37

ВИНИТИ 341.49.37.15
Рубрики: РАДИОФАРМПРЕПАРАТЫ
ЙОД-125
IBVM
СТЕРЕОИЗОМЕРЫ
РАСПРЕДЕЛЕНИЕ В ОРГАНИЗМЕ
ГОЛОВНОЙ МОЗГ
СИГМА-РЕЦЕПТОРЫ

Доп.точки доступа:
Jung, Y.-W.; Mukhopadhyay, S.; Sherman, P.S.; Frey, K.A.; Wieland, D.M.

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