AM-087
Izgled
(IUPAC) ime | |||
---|---|---|---|
(6aR,10aR)-3-(2-metil-6-bromoheks-2-il)-6,6,9-trimetil-6a,7,10,10a-tetrahidrobenzo[c]hromen-1-ol | |||
Klinički podaci | |||
Identifikatori | |||
ATC kod | ? | ||
PubChem[1][2] | 10717065 | ||
ChemSpider[3] | 8892405 | ||
ChEMBL[4] | CHEMBL199561 | ||
Hemijski podaci | |||
Formula | C23H33BrO2 | ||
Mol. masa | 421,410 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
AM-087 je analgetski lek koji deluje kao kanabinoidni agonist. On je derivat Δ8THC supstituisanog u 3-poziciji bočnog lanca. AM-087 je potentan CB1 agonist sa Ki od 0,43 nM, te je oko 100x potentniji od THC. Dodatna aktivnost je verovatno posledica glomaznog bromnog supstituenta na bočnom lancu.[5][6][7]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.
- ↑ Charalambous A, et al. Pharmacological evaluation of halogenated delta 8-THC analogs. Pharmacology, Biochemistry and Behaviour. 1991 Nov;40(3):509-12. PMID 1666915
- ↑ Nikas SP, et al. The role of halogen substitution in classical cannabinoids: a CB1 pharmacophore model. AAPS Journal. 2004 Oct 19;6(4):e30. PMID 15760095
- ↑ Roger Pertwee. Cannabinoids. Handbook of Experimental Pharmacology Volume 168, p 269. Springer. ISBN 3-540-22565-X