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Umespirone

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Umespirone

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Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. 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). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.

Chemical data

Formula
C28H40N4O5
Molecular weight
512.6 g/mol
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
SMILES
CCCCN1C(=O)C2C(=O)N(C(=O)C(C1=O)C2(C)C)CCCCN3CCN(CC3)C4=CC=CC=C4OC
InChIKey
BXNRTMZZILHVNJ-UHFFFAOYSA-N
XLogP
3.4
Polar surface area
90.5 Ų
H-bond donors
0
H-bond acceptors
7
Formal charge
0

via PubChem

Wikidata facts

Mass
512.29987
Show 2 more facts
chemical formula
C₂₈H₄₀N₄O₅
canonical SMILES
CCCCN1C(=O)C2C(=O)N(C(=O)C(C1=O)C2(C)C)CCCCN3CCN(CC3)C4=CC=CC=C4OC
Sources (2)

via Wikidata · CC0

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Encyclopedic overview

3 sections
Contents
  • Synthesis
  • See also
  • References

Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. 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). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms.

==Synthesis== center|700px|thumb|class=skin-invert-image|Synthesis: Patent:

Excerpted from Wikipedia’s “Umespirone” article, available under the CC BY-SA 4.0 licence.

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