PEPA (drug): Difference between revisions

PEPA (drug)
Clinical data
Other names	PEPA
Legal status
Legal status	Investigational New Medicine;
Identifiers
	IUPAC name 2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}thio)phenoxy]acetamide;
CAS Number	141286-78-4;
PubChem CID	6603828;
CompTox Dashboard (EPA)	DTXSID60424960 ;
Chemical and physical data
Formula	C16H16F2N2O4S2
Molar mass	402.436 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC=C(C=C1)S(=O)(=O)NCCSC2=CC(=C(C(=C2)F)OCC(=O)N)F;
	(verify)

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Revision as of 05:57, 11 July 2011

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

^ 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.
^ 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.
^ 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.
^ Sekiguchi, M; Yamada, K; Jin, J; Hachitanda, M; Murata, Y; Namura, S; Kamichi, S; Kimura, I; Wada, K (2001). "The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment". Neuroreport. 12 (13): 2947–50. PMID 11588608.

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[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.

[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.

[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; Wada, K (2001). "The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment". Neuroreport. 12 (13): 2947–50. PMID 11588608.

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