Olorinab (APD 371) 是大麻素受体 2 型 (CB2) 强有效的、选择性的全激动剂，其对 hCB2 的EC50 值为 6.2 nM。

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.

A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed. Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling[1].

Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). The analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors[1]. In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration.

1268881-20-4

C18H23N5O3

357.41

APD 371

DMSO:180mg/mL (503.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years