Dekstrorfan
IUPAC ime | |
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(+)-17-methyl- 9a,13a,14a-morphinan- 3-ol | |
Pravni status | |
Pravni status |
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Identifikatori | |
CAS broj | 125-73-5 Y |
ATC kod | none |
PubChem | CID 5360697 |
Hemijski podaci | |
Formula | C17H23NO |
Molarna masa | 257.371 g/mol |
Dekstrorfan (DXO) je psihoaktivni lek iz morfinanske hemijske klase koji deluje kao antitusivni lek (supresant kašlja) i disocijativni halucinogen. On je dekstro-stereoizomer racemorfana, gde je leva-polovina levorfanol. Dekstrorfan se proizvodi O-demetilacijom dekstrometorfana CYP2D6-om. Dekstrorfan je NMDA antagonist i doprinosi riziku zloupotrebe dekstrometorfana.[1]
Farmakologija
- Nekompetitivni antagonist N-metil-D-aspartatnog receptora (NMDAR).[2][3][4]
- Agonist σ1 i σ2 sigma receptora.[5][6]
- Antagonist α3β4, α4β2, i α7 nikotinskog acetilholinskog receptora.[7][8]
- Bloker L-tip naponom-kontrolisanog kalcijumskog kanala (LVGCC).[4][9]
Reference
- ^ Zawertailo, LA; Kaplan, HL; Busto, UE; Tyndale, RF; Sellers, EM (1998). „Psychotropic effects of dextromethorphan are altered by the CYP2D6 polymorphism: a pilot study”. Journal of clinical psychopharmacology. 18 (4): 332—7. PMID 9690700.
- ^ Wong BY, Coulter DA, Choi DW, Prince DA (1988). „Dextrorphan and dextromethorphan, common antitussives, are antiepileptic and antagonize N-methyl-D-aspartate in brain slices”. Neuroscience Letters. 85 (2): 261—6. PMID 2897648. doi:10.1016/0304-3940(88)90362-X.
- ^ Church J, Jones MG, Davies SN, Lodge D (1989). „Antitussive agents as N-methylaspartate antagonists: further studies”. Canadian Journal of Physiology and Pharmacology. 67 (6): 561—7. PMID 2673498.
- ^ а б Kamel IR, Wendling WW, Chen D, Wendling KS, Harakal C, Carlsson C (2008). „N-methyl-D-aspartate (NMDA) antagonists--S(+)-ketamine, dextrorphan, and dextromethorphan--act as calcium antagonists on bovine cerebral arteries”. Journal of Neurosurgical Anesthesiology. 20 (4): 241—8. PMID 18812887. doi:10.1097/ANA.0b013e31817f523f. Архивирано из оригинала 18. 07. 2011. г. Приступљено 06. 05. 2011.
- ^ Richter A, Löscher W (1997). „Dextrorphan, but not dextromethorphan, exerts weak antidystonic effects in mutant dystonic hamsters”. Brain Research. 745 (1-2): 336—8. PMID 9037429. doi:10.1016/S0006-8993(96)01254-1.
- ^ Chou YC, Liao JF, Chang WY, Lin MF, Chen CF (1999). „Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan”. Brain Research. 821 (2): 516—9. PMID 10064839. doi:10.1016/S0006-8993(99)01125-7.
- ^ Damaj MI, Flood P, Ho KK, May EL, Martin BR (2005). „Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity”. The Journal of Pharmacology and Experimental Therapeutics. 312 (2): 780—5. PMID 15356218. doi:10.1124/jpet.104.075093.
- ^ Hernandez SC, Bertolino M, Xiao Y, Pringle KE, Caruso FS, Kellar KJ (2000). „Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors”. J. Pharmacol. Exp. Ther. 293 (3): 962—7. PMID 10869398.
- ^ Kim HC; Ko KH; Kim WK; et al. (2001). „Effects of dextromethorphan on the seizures induced by kainate and the calcium channel agonist BAY k-8644: comparison with the effects of dextrorphan”. Behavioural Brain Research. 120 (2): 169—75. PMID 11182165. doi:10.1016/S0166-4328(00)00372-7. CS1 одржавање: Експлицитна употреба et al. (веза)
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Grupa I | Agonisti: Neselektivni: ACPD • DHPG • Kuiskualinska kiselina; mGlu1-selektivni: Ro01-6128 • Ro67-4853 • Ro67-7476 • VU-71; mGlu5-selektivni: ADX-47273 • CDPPB • CHPG • DFB • VU-1545 Antagonisti: Neselektivni: MCPG • NPS-2390; mGlu1-selektivni: BAY 36-7620 • CPCCOEt • LY-367,385 • LY-456,236; mGlu5-selektivni: DMeOB • Fenobam • LY-344,545 • MPEP • MTEP • SIB-1757 • SIB-1893 |
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Grupa II | Agonisti: Neselektivni: CBiPES • DCG-IV • Eglumegad • LY-379,268 • LY-404,039 • LY-487,379 • MGS-0028; mGlu2-selektivni: BINA • LY-566,332 Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3-selektivni: CECXG; Negativni alosterni modulatori: RO4491533 |
Grupa III | Agonisti: Neselektivni: L-AP4; mGlu4-selektivni: PHCCC • VU-001,171 • VU-0155,041; mGlu7-selektivni: AMN082; mGlu8-selektivni: DCPG Antagonisti: Neselektivni: CPPG • MAP4 • MSOP • MPPG • MTPG • UBP-1112; mGlu7-selektivni: MMPIP |
transporta
EAAT | |
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vGluT |
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