Ensaculin

Ensaculin (KA-672) is a drug from the coumarin family, which has been researched as a potential treatment for dementia. It acts on a number of receptor systems, being both a weak NMDA antagonist and a 5HT1A agonist.[1][2] Animal studies have shown promising nootropic effects,[3][4] although efficacy in humans has yet to be proven. It was well tolerated in human trials, with the main side effect being orthostatic hypotension (low blood pressure).[5]

Ensaculin
Clinical data
ATC code
  • none
Pharmacokinetic data
Elimination half-life13.7 hours
Identifiers
IUPAC name
  • 7-methoxy-6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propoxy]-3,4-dimethylchromen-2-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC26H32N2O5
Molar mass452.543 g·mol−1
3D model (JSmol)
SMILES
  • O=C/4Oc3cc(OC)c(OCCCN2CCN(c1ccccc1OC)CC2)cc3\C(=C\4C)C
InChI
  • InChI=1S/C26H32N2O5/c1-18-19(2)26(29)33-23-17-24(31-4)25(16-20(18)23)32-15-7-10-27-11-13-28(14-12-27)21-8-5-6-9-22(21)30-3/h5-6,8-9,16-17H,7,10-15H2,1-4H3 N
  • Key:FQELZLMTAPJJOL-UHFFFAOYSA-N N
 NY (what is this?)  (verify)

See also

References
  1. Lishko PV, Maximyuk OP, Chatterjee SS, Nöldner M, Krishtal OA (December 1998). "The putative cognitive enhancer KA-672.HCl is an uncompetitive voltage-dependent NMDA receptor antagonist". NeuroReport. 9 (18): 4193–7. doi:10.1097/00001756-199812210-00035. PMID 9926872. S2CID 29960822.
  2. Winter JC, Helsley SE, Rabin RA (July 1998). "The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component". Pharmacology, Biochemistry, and Behavior. 60 (3): 703–7. doi:10.1016/S0091-3057(98)00043-4. PMID 9678654. S2CID 6493994.
  3. Hoerr R, Noeldner M (2002). "Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment". CNS Drug Reviews. 8 (2): 143–58. doi:10.1111/j.1527-3458.2002.tb00220.x. PMC 6741668. PMID 12177685.
  4. Knauber J, Müller WE (March 2003). "Anseculin improves passive avoidance learning of aged mice". Pharmacological Research. 47 (3): 225–33. doi:10.1016/S1043-6618(02)00311-0. PMID 12591018.
  5. Sourgens H, Hoerr R, Biber A, Steinbrede H, Derendorf H (April 1998). "KA 672-HCl, a neuronal activator against dementia: tolerability, safety, and preliminary pharmacokinetics after single and multiple oral doses in healthy male and female volunteers". Journal of Clinical Pharmacology. 38 (4): 373–81. doi:10.1002/j.1552-4604.1998.tb04438.x. PMID 9590466. S2CID 32558296.


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