Umespirone

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]

Umespirone
Clinical data
Routes of
administration		oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Pharmacokinetic data
Elimination half-lifeUnknown but effects last much longer than other azapirones, up to 23 hours after a single dose in human clinical studies.[1]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC28H40N4O5
Molar mass512.651 g·mol−1
3D model (JSmol)

See also

References
  1. Holland RL, Wesnes K, Dietrich B (1994). "Single dose human pharmacology of umespirone". European Journal of Clinical Pharmacology. 46 (5): 461–8. doi:10.1007/bf00191912. PMID 7957544.
  2. 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.
  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. 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. 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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