Enadolin
(Preusmjereno sa stranice JMBYBVLCYODBJQ-HFMPRLQTSA-N)
| |||
| (IUPAC) ime | |||
|---|---|---|---|
| 2-(benzofuran-4-yl)-N-methyl-N-((5R,7S,8S)-7-
(pyrrolidin-1-yl)-1-oxaspiro[4.5] decan-8-yl)ethanamide | |||
| Klinički podaci | |||
| Identifikatori | |||
| CAS broj | 124378-77-4 | ||
| ATC kod | nije dodeljen | ||
| PubChem[1][2] | 60768 | ||
| ChemSpider[3] | 54765 | ||
| ChEMBL[4] | CHEMBL318859 
| ||
| Hemijski podaci | |||
| Formula | C24H32N2O3 | ||
| Mol. masa | 396.52 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
Enadolin je lek koji deluje kao visoko selektivni agonist κ-opioidnog receptora.
U ispitivanjima na ljudima je pokazano da proizvodi vizuelne distorzije i osećaje disocijacije, slično efektima salvinorina A.[5] Ispitivan je kao potencijalni analgetik, ali je to obustavljeno zbog pojave disforije na većim dozama, što se može očekivati od κ-opioidnog agonista. Razmatrana je mogućnost njegove primene u lečenju komatoznih povreda glave ili žrtava moždanog udara, gde bi taj tip nuspojave bio nevažan.[6]
Sinteza[uredi | uredi kod]
Hemijska sinteza enadolina je slična sintezi spiradolina, pošto oba jedinjenja imaju isti intermedijar i samo se međusobno razlikuju u pogledu finalnog koraka.[7]
Vidi još[uredi | uredi kod]
Literatura[uredi | uredi kod]
- ↑ 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.
- ↑ Walsh SL, Strain EC, Abreu ME, Bigelow GE (2001). „Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans”. Psychopharmacology (Berl.) 157 (2): 151–62. DOI:10.1007/s002130100788. PMID 11594439.
- ↑ Barber A, Gottschlich R (1997). „Novel developments with selective, non-peptidic kappa-opioid receptor agonists”. Expert Opin Investig Drugs 6 (10): 1351–68. DOI:10.1517/13543784.6.10.1351. PMID 15989506.
- ↑ Halfpenny, Paul R.; Horwell, David C.; Hughes, John; Hunter, John C.; Rees, David C. (1990). „Highly selective .kappa.-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted cyclohexyl]arylacetamide derivatives”. Journal of Medicinal Chemistry 33 (1): 286. DOI:10.1021/jm00163a047. PMID 2153208.
