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PA-8 

目录号: HY-133529
产品使用指南

PA-8 是一种有效的,选择性的,具有口服活性的 PACAP I 型 (PAC1) 受体拮抗剂。PA-8 抑制 PAC1受体中 PACAP 诱导的 CREB 的磷酸化,但不抑制 VPAC1 或 VPAC2 受体。PA-8 还抑制 PACAP 诱导的 cAMP 升高,IC50 为 2 nM。

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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.

References
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PA-8PA8PA 8OthersPACAPcAMPanalgesicsPAC1CREBphosphorylationaversiveinflammatorypainInhibitorinhibitorinhibit

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PA-8
目录号:
HY-133529
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