Camicinal is a selective motilin receptor agonist (pEC50: 7.9).

Camicinal ?had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal ?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 ?were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) . Camicinal ?activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal ?was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .

Camicinal (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;?P1.14 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 ?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) [3].?Camicinal ?strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only .

923565-21-3

C25H33FN4O

424.55

GSK962040;Camicinal

DMSO:100 mg/mL (235.54 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years