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'''JWH-081''' is an [[analgesic]] chemical from the [[naphthoylindole]] family, which acts as a [[cannabinoid]] agonist at both the CB<sub>1</sub> and CB<sub>2</sub> receptors.<ref>Aung MM, Griffin G, Huffman JW, Wu MJ, Keel C, Yang B, Showalter VM, Abood ME, Martin BR. Influence of the N-1 alkyl chain length of cannabimimetic indoles upon CB<sub>1</sub> and CB<sub>2</sub> receptor binding. ''Drug and Alcohol Dependence'' 2000; 60:133-140.</ref> With a [[dissociation constant|K<sub>i</sub>]] of 1.2nM it is fairly selective for the CB<sub>1</sub> subtype, its affinity at this subtype approximately 10x the affinity at CB<sub>2</sub>.<ref>Huffman JW, Zengin G, Wu MJ, Lu J, Hynd G, Bushell K, Thompson ALS, Bushell S, Tartal C, Hurst DP, Reggio PH, Selley DE, Cassidy MP, Wiley JL, Martin BR. Structure–activity relationships for 1-alkyl-3-(1-naphthoyl)indoles at the cannabinoid CB<sub>1</sub> and CB<sub>2</sub> receptors: steric and electronic effects of naphthoyl substituents. New highly selective CB<sub>2</sub> receptor agonists. ''Bioorganic and Medicinal Chemistry''. 2005; 13:89-112.</ref> It was discovered by and named after Dr. [[John W. Huffman]]. |
'''JWH-081''' is an [[analgesic]] chemical from the [[naphthoylindole]] family, which acts as a [[cannabinoid]] agonist at both the CB<sub>1</sub> and CB<sub>2</sub> receptors.<ref>Aung MM, Griffin G, Huffman JW, Wu MJ, Keel C, Yang B, Showalter VM, Abood ME, Martin BR. Influence of the N-1 alkyl chain length of cannabimimetic indoles upon CB<sub>1</sub> and CB<sub>2</sub> receptor binding. ''Drug and Alcohol Dependence'' 2000; 60:133-140.</ref> With a [[dissociation constant|K<sub>i</sub>]] of 1.2nM it is fairly selective for the CB<sub>1</sub> subtype, its affinity at this subtype approximately 10x the affinity at CB<sub>2</sub>.<ref>Huffman JW, Zengin G, Wu MJ, Lu J, Hynd G, Bushell K, Thompson ALS, Bushell S, Tartal C, Hurst DP, Reggio PH, Selley DE, Cassidy MP, Wiley JL, Martin BR. Structure–activity relationships for 1-alkyl-3-(1-naphthoyl)indoles at the cannabinoid CB<sub>1</sub> and CB<sub>2</sub> receptors: steric and electronic effects of naphthoyl substituents. New highly selective CB<sub>2</sub> receptor agonists. ''Bioorganic and Medicinal Chemistry''. 2005; 13:89-112.</ref> It was discovered by and named after Dr. [[John W. Huffman]]. |
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==See also== |
==See also== |
Revision as of 07:58, 25 August 2011
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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.230.181 |
Chemical and physical data | |
Formula | C25H25NO2 |
Molar mass | 371.47 g/mol g·mol−1 |
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JWH-081 is an analgesic chemical from the naphthoylindole family, which acts as a cannabinoid agonist at both the CB1 and CB2 receptors.[2] With a Ki of 1.2nM it is fairly selective for the CB1 subtype, its affinity at this subtype approximately 10x the affinity at CB2.[3] It was discovered by and named after Dr. John W. Huffman.
See also
References
- ^ "Ustawa z dnia 15 kwietnia 2011 r. o zmianie ustawy o przeciwdziałaniu narkomanii ( Dz.U. 2011 nr 105 poz. 614 )". Internetowy System Aktów Prawnych. Retrieved 12 June 2011.
- ^ Aung MM, Griffin G, Huffman JW, Wu MJ, Keel C, Yang B, Showalter VM, Abood ME, Martin BR. Influence of the N-1 alkyl chain length of cannabimimetic indoles upon CB1 and CB2 receptor binding. Drug and Alcohol Dependence 2000; 60:133-140.
- ^ Huffman JW, Zengin G, Wu MJ, Lu J, Hynd G, Bushell K, Thompson ALS, Bushell S, Tartal C, Hurst DP, Reggio PH, Selley DE, Cassidy MP, Wiley JL, Martin BR. Structure–activity relationships for 1-alkyl-3-(1-naphthoyl)indoles at the cannabinoid CB1 and CB2 receptors: steric and electronic effects of naphthoyl substituents. New highly selective CB2 receptor agonists. Bioorganic and Medicinal Chemistry. 2005; 13:89-112.