Johimbin

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Johimbin
(IUPAC) ime
17α-hidroksi-johimban-16α-
metil estar karboksilne kiseline
Klinički podaci
Robne marke Yocon
Identifikatori
CAS broj 146-48-5
ATC kod G04BE04 QV03AB93
PubChem[1][2] 8969
DrugBank DB01392
ChemSpider[3] 8622
UNII 2Y49VWD90Q YesY
ChEBI CHEBI:10093 YesY
ChEMBL[4] CHEMBL15245 YesY
Hemijski podaci
Formula C21H26N2O3 
Mol. masa 354,44 g/mol (baza)
390,90 g/mol (hidrohlorid)
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status OTC
Način primene Oralno

Johimbin je alkaloid sa stimulantnim i afrodizijskim dejstvom koji se prirodno javlja u biljci Pausinystalia yohimbe. On se takođe prirodno javlja u Rauwolfia serpentina i Alchornea floribunda, zajedno sa nekoliko drugih alkaloida. Johimbin je korišten kao dijetarni suplement u obliku biljnog ekstrakta i kao lek na recepat u čistoj formi za tretman seksualne disfunkcije. Johimbin je izučavan kao lek za tip 2 dijabetes.[5]

Farmakologija[uredi - уреди | uredi kôd]

Johimbin ima visok afinitet za α2-adrenergički receptor, umereni afinitet za α1-adrenergički, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, i D2 receptore, i slab afinitet za 5-HT1E, 5-HT2A, 5-HT5A, 5-HT7, i D3 receptore.[6][7] On deluje kao antagonist na α1-adrenergičkom, α2-adrenergičkom, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, i D2, i kao parcijalni agonist na 5-HT1A.[6][8][9][10]

Reference[uredi - уреди | uredi kôd]

  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. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  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. http://www.jcheminf.com/content/2/1/3.  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. Rosengren, A. H.; Jokubka, R.; Tojjar, D.; Granhall, C.; Hansson, O.; Li, D.-Q.; Nagaraj, V.; Reinbothe, T. M. i dr.. (2009). „Overexpression of Alpha2A-Adrenergic Receptors Contributes to Type 2 Diabetes”. Science 327 (5962): 217–20. DOI:10.1126/science.1176827. PMID 19965390. 
  6. 6,0 6,1 Millan MJ, Newman-Tancredi A, Audinot V i dr.. (February 2000). „Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states”. Synapse 35 (2): 79–95. DOI:10.1002/(SICI)1098-2396(200002)35:2<79::AID-SYN1>3.0.CO;2-X. PMID 10611634. 
  7. „PDSP Ki Database”. Arhivirano iz originala 2013-11-08. https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php#search. 
  8. 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. 
  9. 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. 
  10. Baxter GS, Murphy OE, Blackburn TP (May 1994). „Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle”. British Journal of Pharmacology 112 (1): 323–31. PMC 1910288. PMID 8032658. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1910288/. 

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