Umespirone

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Umespirone
File:Umespirone skeletal.svg
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
Routes of
administration
oral
Legal status
Legal status
  • uncontrolled
Pharmacokinetic data
Biological 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
Chemical data
Formula C28H40N4O5
Molar mass 512.64 g/mol[[Script error: No such module "String".]]
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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

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  1. 1.0 1.1 Holland RL, Wesnes K, Dietrich B (1994). "Single dose human pharmacology of umespirone". European Journal of Clinical Pharmacology. 46 (5): 461–8. PMID 7957544. 
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  5. 5.0 5.1 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. 
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