1436004-46-4

1436004-46-4 structure
1436004-46-4 structure
  • Name: PA-9
  • Chemical Name: PA-9
  • CAS Number: 1436004-46-4
  • Molecular Formula: C17H18N6O2
  • Molecular Weight: 338.36
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2022-03-11 17:04:58
  • Modify Date: 2025-08-25 12:29:18
  • 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].

Name PA-9
Description 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].
Related Catalog
Target

PAC1 receptor

In Vitro 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].
In Vivo 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]. Animal Model: Male ddY mice (6 weeks old at the start of experiments; intrathecal injection 100 pmol/5 μL PACAP)[1] Dosage: intrathecal injection, co-injection with PACAP. Administration: 100 pmol/5 μL Result: Attenuated the development of PACAP-induced aversive responses. Blocked the induction of PACAP-induced mechanical allodynia.
References

[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.

Molecular Formula C17H18N6O2
Molecular Weight 338.36
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