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Pharmacological comparison of the alternatively spliced short and long CCK 2 receptors
Author(s) -
Morton M F,
Harper E A,
Tavares I A,
Shankley N P
Publication year - 2003
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0705423
Subject(s) - cholecystokinin , receptor , radioligand , cholecystokinin receptor , radioligand assay , antagonist , gene isoform , receptor antagonist , biology , cholecystokinin b receptor , chemistry , pharmacology , medicine , biochemistry , gene
The alternatively spliced, short and long cholecystokinin receptors (CCK 2S and CCK 2L ) were expressed in NIH3T3 cells, and compared using radioligand‐binding assays with identical buffer and incubation conditions. As judged by a saturation analysis, the selective CCK 2 ‐receptor antagonist radioligand [ 3 H]‐JB93182 did not discriminate between the CCK 2S or CCK 2L receptors. A global analysis of competition studies, using a range of structurally diverse, CCK‐receptor selective ligands, provided further evidence that these receptor subtypes were pharmacologically indistinguishable. However, when analysed individually a number of small, yet significant differences were observed with some of the compounds. These data are consistent with previous study that suggested a possible pharmacological difference between these isoforms, at least in terms of the CCK 2 ‐receptor antagonist, L‐365,260. However, it would appear that the pharmacological profile of these compounds is not consistent with their affinity at the putative G 1 /G 2 receptors previously described by Harper et al.British Journal of Pharmacology (2003) 140 , 218–224. doi: 10.1038/sj.bjp.0705423