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PA-8 

Cat. No.: HY-133529
Handling Instructions

PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.

For research use only. We do not sell to patients.

PA-8 Chemical Structure

PA-8 Chemical Structure

CAS No. : 878437-15-1

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Description

PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM[1][2].

In Vitro

In PAC1/CHO cells, PA-8 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP (1 nM)-induced CREB phosphorylation. In VPAC1/CHO and VPAC2/CHO cells, PACAP (1 nM) also induced CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit PACAP (1 nM)-induced CREB phosphorylation[1].

In Vivo

PA-8 (100 pmol/5 µL; intrathecal injection; once; male ddY mice) treatment inhibits PACAP-induced aversive responses and mechanical allodynia in vivo[1].
PA-8 (3-30 mg/kg, p.o.) treatment results in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. PA-8 also inhibits c-fos upregulation in the ipsilateral dorsal horn of the spinal cord[2].

Animal Model: Male ddY mice (6 weeks old) injected with PACAP (100 pmol)[1]
Dosage: 100 pmol/5 µL
Administration: Intrathecal injection; once
Result: Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.
Molecular Weight

342.35

Formula

C₁₇H₁₈N₄O₄

CAS No.

878437-15-1

SMILES

O=C1C(C(C2=CC=C(OCC=C)C(OC)=C2)CC(N3)=O)=C3N=C(N)N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PA-8PA8PA 8OthersPACAPcAMPanalgesicsPAC1CREBphosphorylationaversiveinflammatorypainInhibitorinhibitorinhibit

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