For research use only. Not for therapeutic Use.
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1].
PA-9 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP-induced (1 nM) CREB phosphorylation in the CHO cells expressing PAC1 receptors[1].
PA-9 (100 pmol; co-injection with PACAP) attenuates the development of PACAP-induced (100 pmol/5 μL; intrathecal injection) aversive responses of mice[1].
PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia[1].
PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice[1].
PA-9 is well accommodated in the subpocket formed by L80, F81, I83, G91, V92, P107, A112, and C113 of the PAC1 receptor, precipitating in hydrophobic interactions[1].
Catalog Number | I034143 |
CAS Number | 1436004-46-4 |
Synonyms | N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide |
Molecular Formula | C17H18N6O2 |
Purity | ≥95% |
InChI | InChI=1S/C17H18N6O2/c24-15-7-11(17(25)19-6-5-12-8-18-10-20-12)9-23(15)16-13-3-1-2-4-14(13)21-22-16/h1-4,8,10-11H,5-7,9H2,(H,18,20)(H,19,25)(H,21,22) |
InChIKey | WWPHFXOMYQJGGF-UHFFFAOYSA-N |
SMILES | C1C(CN(C1=O)C2=NNC3=CC=CC=C32)C(=O)NCCC4=CN=CN4 |
Reference | [1]. Takasaki I, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8. |