- 英文名称
- Olorinab
- 分子式
- C18H23N5O3
- 分子量
- 357.41
- 中文别名
- 化合物T14302; 化合物OLORINAB; (4AS,5AS)-4,4A,5,5A-四氢-N-[(1S)-1-(羟甲基)-2,2-二甲基丙基]-1-(4-氧代-2-吡嗪基)-1H-环丙烷并[4,5]环戊二烯并[1,2-C]吡唑-3-甲酰胺; 3-[(4AS,5AS)-3-[[(S)-1-羟基-3,3-二甲基-2-丁基]氨基甲酰基]-4,4A,5,5A-四氢-1H-环丙并[4,5]环戊并[1,2-C]吡唑-1-基]吡嗪-1-氧化物; 3-((4AS,5AS)-3-(((S)-1-羟基-3,3-二甲基丁烷-2-基)氨基甲酰基)-4,4A,5,5A-四氢-1H-环丙并[4,5]环戊二烯并[1,2-C]吡唑-1-基)吡嗪 1-氧化物; 1H-Cyclopropa[4,5]cyclopenta[1,2-c]pyrazole-3-carboxamide, 4,4a,5,5a-tetrahydro-N-[(1S)-1-(hydroxymethyl)-2,2-dimethylpropyl]-1-(4-oxido-2-pyrazinyl)-, (4aS,5aS)-; APD 371; (2S,4S)-N-[(1S)-1-(hydroxymethyl)-2,2-dimethyl-propyl]-9-(4-oxidopyrazin-4-ium-2-yl)-8,9-diazatricyclo[4.3.0.02?]nona-1(6),7-diene-7-carboxamide; 3-[(4aS,5aS)-3-[[(S)-1-Hydroxy-3,3-dimethyl-2-butyl]carbamoyl]-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl]pyrazine 1-Oxide; 3-((4aS,5aS)-3-(((S)-1-Hydroxy-3,3-dimethylbutan-2-yl)carbamoyl)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl)pyrazine 1-oxide
- 用途
- - 生物活性
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。
- 靶点
EC50: 6.2 nM (hCB
2
).
- 体外研究
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, and that Olorinab (APD 371) is highly selective for CB
2
over CB
1
in both binding and functional assays. Furthermore, Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB
2
suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling.
- 体内研究
Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED
50
=2.3 mg/kg). 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. Seperately, the analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB
2
receptors.
