GSK962040

Research use only, not for human use.

A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R).

A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG.channel; possesses highly excellent pharmacokinetic profiles in both rat and dog.Other indication Phase 2 Clinical.

Camicinal (GSK962040) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal (GSK962040) 300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and Camicinal (GSK962040) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) . Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal (GSK962040) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .

Camicinal (GSK962040) (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) . Camicinal (GSK962040) induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >1.14 μmol L 1. After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) . he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%. Camicinal (GSK962040) shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) . Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only .

Camicinal | GSK 962040 | GSK-962040

GPCR/G Protein

Motilin Receptor

Motilin Receptor

Other Indications

Other Disease

923565-21-3

424.5541

C25H33FN4O

>98% (HPLC)

DMSO: 12.73 mg/mL (Need ultrasonic)

CC1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F

Ethanone, 1-[4-[(3-fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years