title: Pharmacological comparison of the alternatively spliced short and long CCK2 receptors.
abstract: (1) The alternatively spliced, short and long cholecystokinin receptors (CCK2S and CCK2L) were expressed in NIH3T3 cells, and compared using radioligand-binding assays with identical buffer and incubation conditions. (2) As judged by a saturation analysis, the selective CCK2-receptor antagonist radioligand [3H]-JB93182 did not discriminate between the CCK2S or CCK2L receptors. (3) 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. (4) These data are consistent with previous study that suggested a possible pharmacological difference between these isoforms, at least in terms of the CCK2-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 G1/G2 receptors previously described by Harper et al.
authors.affiliation: Academic Department of Surgery, GKT Schools of Medicine and Dentistry, King's College, London SE5 9NU. mmorton1@pdus.jnj.com
authors.forename: M F
authors.initials: MF
authors.lastname: Morton
authors.forename: E A
authors.initials: EA
authors.lastname: Harper
authors.forename: I A
authors.initials: IA
authors.lastname: Tavares
authors.forename: N P
authors.initials: NP
authors.lastname: Shankley
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007211:Indoles / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D041681:NIH 3T3 Cells; D011485:Protein Binding; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*
chemical_list: D007211:Indoles; C109753:JB93182; D043887:Receptor, Cholecystokinin B