PA-9,1436004-46-4

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PA-9

CAS No. : 1436004-46-4

MCE 国际站：PA-9

产品活性：PA-9 是一种垂体腺苷酸环化酶激活多肽 (PACAP) I 型 (PAC1) 受体拮抗剂。PA-9 剂量依赖性地抑制 PACAP 诱导的 cAMP 升高，IC₅₀ 为 5.6 nM。PA-9 可用于研究神经性和/或炎症性疼痛。

研究领域：Others

作用靶点：Others

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.

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.
PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia.
PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice.
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.

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