| 名称 | PA-8 |
| 描述 | PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo. |
| 体外活性 | 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 induces CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit this effect [1]. |
| 体内活性 | Treatment with PA-8 (100 pmol/5 μL; via intrathecal injection; single dose; in male ddY mice) effectively suppresses PACAP-induced aversive reactions and mechanical allodynia in vivo [1]. Additionally, oral administration of PA-8 (3-30 mg/kg) leads to a dose-dependent reduction in the second phase of formalin-induced pain responses. PA-8 also significantly reduces c-fos expression in the spinal cord's ipsilateral dorsal horn [2]. This showcases PA-8's potential in mitigating nociceptive behaviors and neuronal activation in a PACAP-administered male ddY mouse model (6 weeks old; 100 pmol PACAP) [1], confirming its analgesic and anti-allodynic effects in vivo. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended.
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| 关键字 | PA 8 | PA-8 | PA8 |
| 相关产品 | PACAP 1-38 acetate | PACAP (6-38), human, ovine, rat acetate | PAC1R antagonist 1 | PACAP-38 (31-38), human, mouse, rat acetate | PACAP-related Peptide (human) (trifluoroacetate salt) | PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt) | PACAP (1-27), human, ovine, rat acetate | PACAP-related Peptide (rat) (trifluoroacetate salt) | PACAP (1-38), human, ovine, rat |
| 相关库 | 经典已知活性库 | 已知活性化合物库 |
United States
