产品
编 号：F755950
分子式：C27H45NO3
分子量：431.65
分子式：C27H45NO3
分子量：431.65
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CAS No: 2772949-38-7
产品详情
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.
体内研究：
CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) hasa stronger antinociceptive activity.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.Animal Model:Male CD-1 outbred mice
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.
体外研究：
CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively.CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membraneswith an EC50 value of 15.09 nM.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.
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.
体内研究：
CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) hasa stronger antinociceptive activity.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.Animal Model:Male CD-1 outbred mice
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.
体外研究：
CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively.CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membraneswith an EC50 value of 15.09 nM.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.
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