Umespiron

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Umespiron
(IUPAC) ime
3-butil-7-[4-[4-(2-metoksifenil)piperazin-1-il]butil]-9,9-dimetil-3,7-diazabiciklo[3.3.1]nonan-2,4,6,8-tetron
Klinički podaci
Identifikatori
CAS broj 107736-98-1
ATC kod nije dodeljen
PubChem[1][2] 65902
ChemSpider[3] 59311
UNII FG0A3VRL5K YesY
Hemijski podaci
Formula C28H40N4O5 
Mol. masa 512,64 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije Nepoznato ali efekti traju znatno duže od drugih azapirona, do 23 nakon jedne doze u ljudskim kliničkim studijama.[4]
Farmakoinformacioni podaci
Trudnoća ?
Pravni status nije kontrolisan
Način primene oralno

Umespiron (KC-9172) je lek iz azapironske klase koji poseduje anksiolitičke i antipsihotičke osobine.[5][6][7][8] On je parcijalni agonist 5-HT1A receptora (Ki = 15 nM), D2 receptora (Ki = 23 nM), i antagonist α1-adrenoceptora (Ki = 14 nM). On isto tako ima slab afinitet za sigma receptor (Ki = 558 nM).[5][9][10] Za razliku od drugih anksiolitika i antipsihotika, umespiron proizvodi minimalnu sedaciju, kognitivni deficit, katalepsiju, i ekstrapiramidalne simptome.[4][8][9]

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. 4,0 4,1 Holland RL, Wesnes K, Dietrich B (1994). „Single dose human pharmacology of umespirone”. European Journal of Clinical Pharmacology 46 (5): 461–8. PMID 7957544. 
  5. 5,0 5,1 Barnes NM, Costall B, Domeney AM, et al. (September 1991). „The effects of umespirone as a potential anxiolytic and antipsychotic agent”. Pharmacology, Biochemistry, and Behavior 40 (1): 89–96. DOI:10.1016/0091-3057(91)90326-W. PMID 1685786. http://linkinghub.elsevier.com/retrieve/pii/0091-3057(91)90326-W. 
  6. Ruhland M, Krähling H, Fuchs A, Schön U (November 1988). „KC 9172 (free base of KC 7218)--an antipsychotic/anxiolytic compound. I. Antipsychotic and anxiolytic activity in comparison with chlorpromazine, clozapine, diazepam and buspirone”. Pharmacopsychiatry 21 (6): 396–8. DOI:10.1055/s-2007-1017024. PMID 2907649. 
  7. Krähling H, Fuchs A, Ruhland M, Schön U, Mol F, Tulp M (November 1988). „KC 9172 (free base of KC 7218)--an antipsychotic/anxiolytic compound. II. Discrimination from typical neuroleptics and benzodiazepine-like minor tranquilizers”. Pharmacopsychiatry 21 (6): 399–401. DOI:10.1055/s-2007-1017025. PMID 2907650. 
  8. 8,0 8,1 Schmidt WJ, Krähling H, Ruhland M (1991). „Antagonism of AP-5-induced sniffing stereotypy links umespirone to atypical antipsychotics”. Life Sciences 48 (6): 499–505. DOI:10.1016/0024-3205(91)90464-M. PMID 1671523. 
  9. 9,0 9,1 Ahlenius S, Wijkström A (November 1992). „Mixed agonist-antagonist properties of umespirone at neostriatal dopamine receptors in relation to its behavioral effects in the rat”. European Journal of Pharmacology 222 (1): 69–74. DOI:10.1016/0014-2999(92)90464-F. PMID 1361441. 
  10. Itzhak Y, Ruhland M, Krähling H (February 1990). „Binding of umespirone to the sigma receptor: evidence for multiple affinity states”. Neuropharmacology 29 (2): 181–4. DOI:10.1016/0028-3908(90)90058-Y. PMID 1970425. 

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