1268881-20-4
1268881-20-4 structure
- Name: Olorinab
- Chemical Name: APD 371
- CAS Number: 1268881-20-4
- Molecular Formula: C18H23N5O3
- Molecular Weight: 357.41
- Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
- Create Date: 2019-02-09 18:43:36
- Modify Date: 2024-01-10 21:24:21
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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.
| Name | APD 371 |
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| Description | 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. |
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| Related Catalog | |
| Target |
EC50: 6.2 nM (hCB2)[1]. |
| In Vitro | A comprehensive in vitro profile of APD 371 (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed, and that APD 371 is highly selective for CB2 over CB1 in both binding and functional assays. Furthermore, 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, APD 371 would be able to drive agonist-induced receptor recycling[1]. |
| In Vivo | APD 371 significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). In a separate experiment, a single dose of APD 371 (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. Seperately, the analgesic effects of APD 371 are shown to be highly likely mediated via activity at CB2 receptors[1]. |
| References |
| Molecular Formula | C18H23N5O3 |
|---|---|
| Molecular Weight | 357.41 |