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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
Nomenclature CCK1 receptor CCK2 receptor
HGNC, UniProt CCKAR, P32238 CCKBR, P32239
Principal transduction Gq/11/Gs Gs
Rank order of potency CCK-8 >> gastrin-17, CCK-8 (desulphated) > CCK-4 CCK-8 ≥ gastrin-17, CCK-8 (desulphated), CCK-4
Endogenous agonists (pKi) – CCK-8 (desulphated) (pIC50 8.3 – 8.7) [14], CCK-4 (pIC50 7.5) 636
Selective agonists (pKi) A-71623 (pIC50 8.4 - Rat) [2], JMV180 (pIC50 8.3) 639, GW-5823 (pIC50 7.6) 633 RB-400 (9.1 - Rat) [3], PBC-264 (pIC50 9.1 – Rat) 638, gastrin-17 (pIC50 8.3 - Mouse) 634
Selective antagonists (pKi) devazepide (pIC50 9.7 - Rat) [8], T-0632 (pIC50 9.6 - Rat) 650, PD-140548 (pIC50 8.6 - Rat) 647, lintitript (pIC50 8.3) 632, lorglumide (pIC50 6.7 – 8.2 - Rat) 634,637 YF-476 (pIC50 9.7) [4,24], GV150013 (pIC50 9.4) 651, L-740093 (pIC50 9.2) 643, YM-022 (pIC50 9.2) 643, JNJ-26070109 (pIC50 8.5) 642, L-365260 (pIC50 8.4) 640, RP73870 (pIC50 8.0 - Rat) 641, LY262691 (pIC50 7.5 - Rat) 646
Radioligands(Kd) [3H]devazepide (Antagonist) (2x10-10 M) [5] [3H]L365260 (Antagonist) (2.9x10-9 – 5.7x10-9 M) [17], [3H]PD140376 (Antagonist) (Ki 1x10-10 – 2x10-10 M – Guinea pig) 635, [125I]PD142308 (Antagonist) (Ki 2.5x10-10 M), [125I]-BDZ2 (Antagonist) (Ki 3.98x10-9 M) 631, [125I]DTyr-Gly-[(Nle28,31)CCK-26-33 (Agonist, Full agonist) (IC50 1x10-9 M) 645, [125I]gastrin (Agonist, Full agonist) (IC50 1x10-9 M), [3H]gastrin (Agonist, Full agonist) (IC50 1x10-9 M)