amidases

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

AA26-9 is an effective and broad-spectrum inhibitor of serine hydrolase.

Amidases, belonging to the nitrilase superfamily, catalyze amide hydrolysis to yield carboxylic acid and ammonia. These enzymes feature a conserved AS sequence of about 130 amino acids and are pivotal in essential metabolic processes [1].

6-Bn-cAMP is a selective activator of cAMP-dependent protein kinase (PKA) that does not activate Epac. Compared to cAMP, 6-Bn-cAMP enhances hydrolytic stability against PDE, esterases, and amidases, and significantly increases membrane permeability.