Rauvolscin

Из Википедије, слободне енциклопедије
Rauvolscin
(IUPAC) ime
metil estar 17α-hidroksi-20α-johimban-16β-karboksilne kiseline
Klinički podaci
Identifikatori
CAS broj 131-03-3 6211-32-1 (HCl)
ATC kod nije dodeljen
PubChem[1][2] 643606
ChemSpider[3] 558737
ChEBI CHEBI:48562 YesY
ChEMBL[4] CHEMBL10347 YesY
Hemijski podaci
Formula C21H26N2O3 
Mol. masa 354,44 g/mol
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status Nije kontrolisan
Način primene Oralno

Rauvolscin (izojohimbin, α-johimbin, i korinantidin) je alkaloid koji je prisutan kod više vrsta biljki iz rodova Rauwolfia i Pausinystalia.[5] On je stereoizomer johimbina.[5] Rauvolscin je stimulant centralnog nervnog sistema, lokalni anestetik i u izvesnoj meri afrodizijak.[5]

Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[6] On takođe deluje kao parcijalni agonist 5-HT1A receptora i antagonist 5-HT2A i 5-HT2B receptora.[7][8][9]

Reference[уреди]

  1. ^ 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.  edit
  2. ^ 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. 
  3. ^ 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.  edit
  4. ^ 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.  edit
  5. ^ а б в KOHLI JD, DE NN (June 1956). „Pharmacological action of rauwolscine“. Nature 177 (4521): 1182. DOI:10.1038/1771182a0. PMID 13334509. 
  6. ^ Perry BD, U'Prichard DC (December 1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors“. European Journal of Pharmacology 76 (4): 461–4. DOI:10.1016/0014-2999(81)90123-0. PMID 6276200. 
  7. ^ Arthur JM, Casañas SJ, Raymond JR (June 1993). „Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors“. Biochemical Pharmacology 45 (11): 2337–41. DOI:10.1016/0006-2952(93)90208-E. PMID 8517875. 
  8. ^ Kaumann AJ (June 1983). „Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors“. Naunyn-Schmiedeberg's Archives of Pharmacology 323 (2): 149–54. DOI:10.1007/BF00634263. PMID 6136920. 
  9. ^ Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). „[3HRauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor“]. Naunyn-Schmiedeberg's Archives of Pharmacology 357 (1): 17–24. DOI:10.1007/PL00005133. PMID 9459568. 

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