l-797591

Description: L-797, 591 is a novel, potent, selective and nonpeptidyl agonist of SSTR1 (somatostatin receptor subtype 1). L-797, 591 inhibited forskolin-stimulated cAMP accumulation in aconcentration-dependent fashion, with EC(50)s (effective concentrationfor 50% maximal response) of 8.0 x 10(-10) M and 7.0 x 10(-10) M, respectively. No similar concentration-dependent effect onforskolin-stimulated cAMP levels was observed with sst(2)-, sst(3)- orsst(4)-selective agonists. Furthermore, L-797, 591inhibited 10(-7) M CRH-induced cAMP in the embryonic neurons. Theseresults are the first evidence demonstrating that sst(1) regulatesintracellular cAMP levels in embryonic neurons and may inhibitCRH-mediated effects in the embryonic cortex.

References: Neuropharmacology. 2001 Mar; 40(4):590-6. doi: 10.1016/s0028-3908(00)00180-5.