Ensaculin

Ensaculin

Clinical data
ATC code	none
Pharmacokinetic data
Biological half-life	13.7 hours
Identifiers
IUPAC name 7-methoxy-6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propoxy]-3,4-dimethylchromen-2-one
CAS Number	155773-59-4
PubChem (CID)	208923
ChemSpider	181019
UNII	869PGR00AT
ChEMBL	CHEMBL1963107
Chemical and physical data
Formula	C26H32N2O5
Molar mass	452.543
3D model (Jmol)	Interactive image
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 Key:FQELZLMTAPJJOL-UHFFFAOYSA-N
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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 5HT_1A 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]

References

1. Lishko, PV; Maximyuk, OP; Chatterjee, SS; Nöldner, M; Krishtal, OA (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.
2. Winter, JC; Helsley, SE; Rabin, RA (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.
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. PMID 12177685.
4. Knauber, J; Müller, WE (2003). "Anseculin improves passive avoidance learning of aged mice". Pharmacological research : the official journal of the Italian Pharmacological Society. 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 (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.