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Umespirone

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Umespirone
Systematic (IUPAC) name
3-butyl-7-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]-9,9-dimethyl-3,7-diazabicyclo[3.3.1]nonane-2,4,6,8-tetrone
Clinical data
Pregnancy cat.  ?
Legal status uncontrolled
Routes oral
Pharmacokinetic data
Half-life Unknown but effects last much longer than other azapirones, up to 23 hours after a single dose in human clinical studies.[1]
Identifiers
CAS number 107736-98-1
ATC code None
PubChem CID 65902
ChemSpider 59311
UNII FG0A3VRL5K YesY
Chemical data
Formula C28H40N4O5 
Mol. mass 512.64 g/mol
SMILES eMolecules & PubChem

Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties.[2][3][4][5] It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor receptor antagonist (Ki = 14 nM), and also has weak affinity for the sigma receptor (Ki = 558 nM).[2][6][7] Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.[1][5][6]

See also

References

  1. ^ a b 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. ^ a b 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ a b 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. 
  6. ^ a b 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. 
  7. ^ 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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