Ensaculin

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Ensaculin
Ensaculin.png
Systematic (IUPAC) name
7-methoxy-6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propoxy]-3,4-dimethylchromen-2-one
Clinical data
Legal status ?
Pharmacokinetic data
Half-life 13.7 hours
Identifiers
CAS number 155773-59-4 YesY
ATC code None
PubChem CID 208923
ChemSpider 181019 N
UNII 869PGR00AT N
ChEMBL CHEMBL1963107 N
Chemical data
Formula C26H32N2O5 
Mol. mass 452.543
 N (what is this?)  (verify)

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]

References[edit]

  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. 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.