A new, highly selective CCK-B receptor radioligand (( super(3)H)(N-methyl-Nle super(28,31))CCK sub(26-23)): Evidence for CCK-B receptor heterogeneity

(N-methyl-Nle super(28,31))CCK sub(26-33) (SNF 8702) is a nonsulfated cholecystokinin octapeptide analog that is highly selective for cholecystokinin-B (CCK-B) receptors. Inhibition studies using ( super(125)I) Bolton-Hunter-labeled CCK-8 show that SNF 8702 has over 4,000-fold greater affinity for C...

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Published inThe Journal of pharmacology and experimental therapeutics Vol. 255; no. 3; pp. 1278 - 1286
Main Authors Knapp, R J, Vaughn, L K, Fang, Su-Nan, Bogert, CL, Yamamura, MS, Hruby, V J, Yamamura, H I
Format Journal Article
LanguageEnglish
Published 01.01.1990
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Summary:(N-methyl-Nle super(28,31))CCK sub(26-33) (SNF 8702) is a nonsulfated cholecystokinin octapeptide analog that is highly selective for cholecystokinin-B (CCK-B) receptors. Inhibition studies using ( super(125)I) Bolton-Hunter-labeled CCK-8 show that SNF 8702 has over 4,000-fold greater affinity for CCK receptor in guinea pig cortex relative to those in guinea pig pancreas. ( super(3)H)SNF 8702 binds to a single site with high affinity in guinea pig cortex, cerebellum, hippocampus and pons-medulla. Of these four tissues, the highest receptor density was measured in the cortex and the lowest in the pons-medulla. The data show that SNF 8702 is a highly selective ligand for CCK-B receptors. Regional variations in the observed binding properties of ( super(3)H)SNF 8702 suggest the presence of CCK-B receptor subtypes.
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ISSN:0022-3565