Cannabinoid Receptor
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
Cannabinoid Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
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| S9413New |
YangoninYangonin is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
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| S3021 |
RimonabantRimonabant是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。 |
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| S2819 |
AM251AM251是大麻素CB1受体拮抗剂，IC50为700 nM，在体内与小鼠脑CB1受体结合。 |
Effect of AM251 treatment on the CORT response to stress. Group-housed and socially isolated rats were intraperitoneally injected with AM251 or vehicle 30 min before exposure to foot-shock stress, and were sacrificed 30 min thereafter. Non-shocked controls were sacrificed 60 min after injection. Data are mean ± SEM of values from 10 rats per group and are expressed as ng/ml of plasma. Data were analyzed by three-way ANOVA (housing × drug treatment × stress conditions) followed by Newman-Keuls post-hoc test. ap<0.01 vs. the respective non-shocked controls; bp < 0.01 vs. group-housed vehicle-treated rats; cp < 0.01 vs. group-housed vehicle-treated + foot-shock rats.
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| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl是一种有效的，选择性cannabinoid receptor CB1拮抗剂，Ki为0.7 nM，比作用于人类CB2受体选择性高10，000倍。Phase 1。 |
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| S8694New |
CID16020046 (CID 16020046)CID16020046是选择性的GPR55拮抗剂，能够抑制GPR55的固有活性，在酵母中IC50为0.15 μM。CID16020046对其他GPCRs、离子通道、激酶和核受体仅具有微弱活性。 |
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| S1544 |
AM1241AM1241是一种选择性的cannabinoid CB2 receptor激动剂，Ki为3.4 nM，比作用于CB1受体选择性高82倍。 |
The expression of cannabinoid receptor type II, Akt, p-Akt, HO-1, Nrf2 in cytosol and Nrf2 in nucleus were detected by Western blot.
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| S2854 |
BML-190BML-190是一种选择性的cannabinoid CB2 receptor逆向激动剂，Ki为435 nM，比作用于CB1受体选择性高50倍。 |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
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| S2778 |
GW842166XGW842166X是一种有效的，高选择性cannabinoid receptor CB2受体激动剂，EC50为63 nM，对CB1受体没有显著的活性。Phase 2。 |
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| S1534 |
Org 27569Org 27569是cannabinoid CB1 receptor变构调节剂，通过增强激动剂亲和力而诱导CB1受体状态改变，且降低逆向激动剂的亲和力。 |
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| S9048New |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S9413New |
YangoninYangonin is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3021 |
RimonabantRimonabant是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。 |
||
| S2819 |
AM251AM251是大麻素CB1受体拮抗剂，IC50为700 nM，在体内与小鼠脑CB1受体结合。 |
Effect of AM251 treatment on the CORT response to stress. Group-housed and socially isolated rats were intraperitoneally injected with AM251 or vehicle 30 min before exposure to foot-shock stress, and were sacrificed 30 min thereafter. Non-shocked controls were sacrificed 60 min after injection. Data are mean ± SEM of values from 10 rats per group and are expressed as ng/ml of plasma. Data were analyzed by three-way ANOVA (housing × drug treatment × stress conditions) followed by Newman-Keuls post-hoc test. ap<0.01 vs. the respective non-shocked controls; bp < 0.01 vs. group-housed vehicle-treated rats; cp < 0.01 vs. group-housed vehicle-treated + foot-shock rats.
|
|
| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl是一种有效的，选择性cannabinoid receptor CB1拮抗剂，Ki为0.7 nM，比作用于人类CB2受体选择性高10，000倍。Phase 1。 |
||
| S8694New |
CID16020046 (CID 16020046)CID16020046是选择性的GPR55拮抗剂，能够抑制GPR55的固有活性，在酵母中IC50为0.15 μM。CID16020046对其他GPCRs、离子通道、激酶和核受体仅具有微弱活性。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1544 |
AM1241AM1241是一种选择性的cannabinoid CB2 receptor激动剂，Ki为3.4 nM，比作用于CB1受体选择性高82倍。 |
The expression of cannabinoid receptor type II, Akt, p-Akt, HO-1, Nrf2 in cytosol and Nrf2 in nucleus were detected by Western blot.
|
|
| S2854 |
BML-190BML-190是一种选择性的cannabinoid CB2 receptor逆向激动剂，Ki为435 nM，比作用于CB1受体选择性高50倍。 |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
|
| S2778 |
GW842166XGW842166X是一种有效的，高选择性cannabinoid receptor CB2受体激动剂，EC50为63 nM，对CB1受体没有显著的活性。Phase 2。 |
||
| S1534 |
Org 27569Org 27569是cannabinoid CB1 receptor变构调节剂，通过增强激动剂亲和力而诱导CB1受体状态改变，且降低逆向激动剂的亲和力。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S9048New |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
