PEPA (drug)

For the process algebra, see PEPA.
PEPA (drug)
Systematic (IUPAC) name
2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}thio)phenoxy]acetamide
Clinical data
Pregnancy cat.  ?
Legal status Investigational New Medicine
Identifiers
CAS number 141286-78-4
ATC code  ?
PubChem CID 6603828
Synonyms PEPA
Chemical data
Formula C16H16F2N2O4S2 
Mol. mass 402.436 g/mol
SMILES eMolecules & PubChem
 Y(what is this?)  (verify)

PEPA is an ampakine drug which acts as an allosteric potentiator of AMPA receptor desensitisation,[1][2] which is up to 100x more potent than aniracetam in vitro.[3] It produces memory-enhancing effects in rats when administered intravenously.[4]

References

  1. ^ Sekiguchi, M; Takeo, J; Harada, T; Morimoto, T; Kudo, Y; Yamashita, S; Kohsaka, S; Wada, K (1998). "Pharmacological detection of AMPA receptor heterogeneity by use of two allosteric potentiators in rat hippocampal cultures". British journal of pharmacology 123 (7): 1294–303. doi:10.1038/sj.bjp.0701707. PMC 1565288. PMID 9579722. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1565288. 
  2. ^ Sekiguchi, M; Nishikawa, K; Aoki, S; Wada, K (2002). "A desensitization-selective potentiator of AMPA-type glutamate receptors". British journal of pharmacology 136 (7): 1033–41. doi:10.1038/sj.bjp.0704804. PMC 1573432. PMID 12145103. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1573432. 
  3. ^ Sekiguchi, M; Fleck, MW; Mayer, ML; Takeo, J; Chiba, Y; Yamashita, S; Wada, K (1997). "A novel allosteric potentiator of AMPA receptors: 4--2-(phenylsulfonylamino)ethylthio--2,6-difluoro-phenoxyaceta mide". Journal of Neuroscience 17 (15): 5760–71. PMID 9221774. 
  4. ^ Sekiguchi, M; Yamada, K; Jin, J; Hachitanda, M; Murata, Y; Namura, S; Kamichi, S; Kimura, I et al. (2001). "The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment". Neuroreport 12 (13): 2947–50. doi:10.1097/00001756-200109170-00038. PMID 11588608. 
Psychostimulants, agents used for ADHD, and nootropics (N06B)
Centrally acting sympathomimetics
Xanthine derivatives
Glutamate receptor
CX-516 • CX-546 • CX-614 • CX-691 • CX-717 • IDRA-21 • LY-404,187 • LY-503,430 • PEPA • S-18986 • Sunifiram • Unifiram
Eugeroics / Benzhydryl compounds
Histamine H3 receptor antagonists
GABAA α5 inverse agonists
Dopamine D1 receptor agonists
α7 nicotinic agonists / PAMs
Prolyl endopeptidase inhibitors
Alpha-adrenergic agonists
Plants
Antioxidants
Stabilized R-(+)-lipoic acid (RLA)
Other psychostimulants and nootropics

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)