| Identification | Back Directory | [Name]
Octanamide, N-cyclopropyl-8-[3-(1,1-dimethylheptyl)-5-methoxyphenoxy]- | [CAS]
2772949-38-7 | [Synonyms]
CB1/2 agonist 4
Octanamide, N-cyclopropyl-8-[3-(1,1-dimethylheptyl)-5-methoxyphenoxy]- | [Molecular Formula]
C27H45NO3 | [MOL File]
2772949-38-7.mol | [Molecular Weight]
431.65 |
| Hazard Information | Back Directory | [Uses]
CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively[1]. | [in vivo]
CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) has a stronger antinociceptive activity[1].
CB1/2 agonist 4 (1, 3 and 4 mg/kg, i.p.) can activate TRPV1 channel and it behaved as a good TRPV1 agonist with an IC50 value of 0.8 μM and EC50 value of 0.12 μM[1]. | Animal Model: | Male CD-1 outbred mice[1] | | Dosage: | 1, 3 and 4 mg/kg | | Administration: | 1, 3 and 4 mg/kg, i.p. | | Result: | Significantly reduced the late phase of formalin-induced nociceptive behaviour in a dose dependent manner and slightly decreased also the first phase of nociceptive response. |
| [References]
[1] Antonella Brizzi, et al. Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. Bioorg Med Chem. 2020 Jun 1;28(11):115513. DOI:10.1016/j.bmc.2020.115513 |
|
|