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Ensaculin
Systematic (IUPAC) name
7-methoxy-6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propoxy]-3,4-dimethylchromen-2-one
Identifiers
CAS number 155773-59-4
ATC code none
PubChem 208923
Chemical data
Formula C 26H32N2O5  
Mol. mass 452.543
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 13.7 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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 othostatic hypotension (low blood pressure).[5]

References

  1. ^ Lishko PV, Maximyuk OP, Chatterjee SS, Nöldner M, Krishtal OA. The putative cognitive enhancer KA-672.HCl is an uncompetitive voltage-dependent NMDA receptor antagonist. Neuroreport. 1998 Dec 21;9(18):4193-7. PMID 9926872
  2. ^ Winter JC, Helsley SE, Rabin RA. The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. Pharmacology, Biochemistry and Behaviour. 1998 Jul;60(3):703-7. PMID 9678654
  3. ^ Hoerr R, Noeldner M. Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Reviews. 2002 Summer;8(2):143-58. PMID 12177685
  4. ^ Knauber J, Müller WE. Anseculin improves passive avoidance learning of aged mice. Pharmacological Research. 2003 Mar;47(3):225-33. PMID 12591018
  5. ^ Sourgens H, Hoerr R, Biber A, Steinbrede H, Derendorf H. 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. 1998 Apr;38(4):373-81. PMID 9590466
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