GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC50 value of 14 µM in GPR88 cAMP functional assay.
GPR88 agonist 2 significantly enhance [35S]GTPγS binding activity (EC50: 8.9 μM) in WT mouse striatal membranes, but GPR88 agonist 2 is inactive in striatal membranes prepared from GPR88 KO mice.[1].
GPR88 agonist 2 (20mg/ml, ip) has a good plasma exposure (Cmax:1670 ng/mL) and acceptable metabolic stability (T1/2:4.66h, CL:21mL/mg/kg)[1].
GPR88 agonist 2 (20mg/ml, ip) has sufficient brain penetration (Cmax:576 ng/mL)[1].
Pharmacokinetic analysis in mice[1]
| 20 mg/kg, ip | Cmax (ng/mL) | T1/2 (h) | CL(mL/min/kg) | B/Pratio |
| plasma | 1670 | 5.6 | 21 | 0.34 |
| brain | 576 | / | / |