2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. CB1/2 agonist 4

CB1/2 agonist 4 是 CB1 完全激动剂和 CB2 部分激动剂，EC50 值分别为 15.09 nM 和 1.16 nM。CB1/2 agonist 4 对 hCB1 和 hCB2 受体也有亲和力，Ki 值分别为 1.1 nM 和 4.2 nM。CB1/2 agonist 4 具有明显的抗伤害感受活性，也可以激活大麻素和 TRPV1 受体，其 IC50 值为 0.8 μM, EC50 值为 0.12 μM。

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CB1/2 agonist 4 Chemical Structure

CB1/2 agonist 4 Chemical Structure

CAS No. : 2772949-38-7

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CB1/2 agonist 4 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

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].

IC50 & Target

Ki: 1.1 nM (hCB1); 4.2 nM (hCB2)[1].
EC50: 15.09 nM (CB1); EC50: 1.16 nM (CB2)[1].
IC50: 0.8 μM, EC50: 0.12 μM (TRPV1)[1].
体外研究
(In Vitro)

CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively[1].
CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membranes with an EC50 value of 15.09 nM[1].
CB1/2 agonist 4 (0.1 mM) is able to slightly stimulate [35S]GTPγS binding to hCB2-CHO cell membranes, behaving as a weak partial agonist to CB2 receptors of 1.16 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CB1/2 agonist 4 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

431.65

Formula

C27H45NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CB1/2 agonist 4 相关分类

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Keywords:

CB1/2 agonist 42772949-38-7Cannabinoid ReceptorCB1 agonistCB2 agonistTRPV1cannabinoidneurologicalInhibitorinhibitorinhibit

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