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Umespiron Reference Vidi još Spoljašnje veze Мени за навигацију107736-98-16590259311FG0A3VRL5K7957544„The effects of umespirone as a potential anxiolytic and antipsychotic agent”168578610.1016/0091-3057(91)90326-W290764910.1055/s-2007-1017024290765010.1055/s-2007-1017025167152310.1016/0024-3205(91)90464-M136144110.1016/0014-2999(92)90464-F197042510.1016/0028-3908(90)90058-Yууууу

АнтипсихотициДопамински агонистиАзапирониПиперазиниФенолни етри


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Umespiron




Из Википедије, слободне енциклопедије






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Umespiron
Umespirone skeletal.svg

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
Način primeneoralno
Pravni status
Pravni status

  • nije kontrolisan


Farmakokinetički podaci
Poluvreme eliminacije
Nepoznato ali efekti traju znatno duže od drugih azapirona, do 23 nakon jedne doze u ljudskim kliničkim studijama.[1]

Identifikatori
CAS broj
107736-98-1 ДаY
ATC kodnone
PubChemCID 65902
ChemSpider59311
UNII
FG0A3VRL5K ДаY
Hemijski podaci
Formula
C28H40N4O5
Molarna masa512,64 g/mol



Umespiron (KC-9172) je lek iz azapironske klase koji poseduje anksiolitičke i antipsihotičke osobine.[2][3][4][5] 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).[2][6][7] Za razliku od drugih anksiolitika i antipsihotika, umespiron proizvodi minimalnu sedaciju, kognitivni deficit, katalepsiju, i ekstrapiramidalne simptome.[1][5][6]



Reference




  1. ↑ 1,01,1 Holland RL, Wesnes K, Dietrich B (1994). „Single dose human pharmacology of umespirone”. European Journal of Clinical Pharmacology. 46 (5): 461—8. PMID 7957544. 


  2. ↑ 2,02,1 Barnes NM; Costall B; Domeney AM; et al. (1991). „The effects of umespirone as a potential anxiolytic and antipsychotic agent”. Pharmacology, Biochemistry, and Behavior. 40 (1): 89—96. PMID 1685786. doi:10.1016/0091-3057(91)90326-W. CS1 одржавање: Експлицитна употреба et al. (веза)


  3. ^ Ruhland M, Krähling H, Fuchs A, Schön U (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. PMID 2907649. doi:10.1055/s-2007-1017024. 


  4. ^ Krähling H, Fuchs A, Ruhland M, Schön U, Mol F, Tulp M (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. PMID 2907650. doi:10.1055/s-2007-1017025. 


  5. ↑ 5,05,1 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. PMID 1671523. doi:10.1016/0024-3205(91)90464-M. 


  6. ↑ 6,06,1 Ahlenius S, Wijkström A (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. PMID 1361441. doi:10.1016/0014-2999(92)90464-F. 


  7. ^ Itzhak Y, Ruhland M, Krähling H (1990). „Binding of umespirone to the sigma receptor: evidence for multiple affinity states”. Neuropharmacology. 29 (2): 181—4. PMID 1970425. doi:10.1016/0028-3908(90)90058-Y. 



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Spoljašnje veze
















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