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Etazolate

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Etazolate
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • Ethyl 1-ethyl-4-[2-(propan-2-ylidene)hydrazinyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxylate
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC14H19N5O2
Molar mass289.339g·mol−1
3D model (JSmol)
  • CCN1C2=NC=C(C(=C2C=N1)NN=C(C)C)C(=O)OCC
  • InChI=1S/C14H19N5O2/c1-5-19-13-10(8-16-19)12(18-17-9(3)4)11(7-15-13)14(20)21-6-2/h7-8H,5-6H2,1-4H3,(H,15,18)
  • Key:OPQRBXUBWHDHPQ-UHFFFAOYSA-N

Etazolate(SQ-20,009,EHT-0202) is ananxiolyticdrugwhich is apyrazolopyridinederivativeand has uniquepharmacologicalproperties.[1][2][3]It acts as apositive allosteric modulatorof theGABAAreceptorat thebarbituratebinding site,[4][5][6][7]as anadenosineantagonistof theA1andA2subtypes,[8]and as aphosphodiesterase inhibitorselective for thePDE4isoform.[9][10][11]It is currently inclinical trialsfor the treatment ofAlzheimer's disease.[12]

See also

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References

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  1. ^Hall JA, Morton I (1999).Concise dictionary of pharmacological agents: properties and synonyms.Kluwer Academic.ISBN0-7514-0499-3.
  2. ^Williams M (May 1983). "Anxioselective anxiolytics".Journal of Medicinal Chemistry.26(5): 619–628.doi:10.1021/jm00359a001.PMID6132997.
  3. ^Williams M, Risley EA (February 1979). "Enhancement of the binding of 3H-diazepam to rat brain membranes in vitro by SQ 20009, A novel anxiolytic, gamma-aminobutyric acid (GABA) and muscimol".Life Sciences.24(9): 833–841.doi:10.1016/0024-3205(79)90367-9.PMID449623.
  4. ^Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits".European Journal of Pharmacology.301(1–3): 207–214.doi:10.1016/0014-2999(96)00066-0.PMID8773466.
  5. ^Davies MF (1996)."The Pharmacology of the Gamma-Aminobutyric Acid System".In Remington G, Baskys A (eds.).Brain mechanisms and psychotropic drugs.Boca Raton: CRC Press.ISBN0-8493-8386-2.
  6. ^Olsen RW, Gordey M (2000)."GABAA Receptor Chloride Ion Channels".In Mishina M, Kurachi Y (eds.).Pharmacology of ionic channel function: activators and inhibitors.Handbook of Experimental Pharmacology. Vol. 147. Berlin: Springer. pp. 499–517.doi:10.1007/978-3-642-57083-4_19.ISBN3-540-66127-1.
  7. ^Olsen RW (1987)."GABA-Drug Interactions".In Jucker E (ed.).Progress in Drug Research.Vol. 31. Boston: Birkhauser. p. 526.ISBN3-7643-1837-6.
  8. ^Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents".Pharmacology, Biochemistry, and Behavior.29(2): 433–441.doi:10.1016/0091-3057(88)90182-7.PMID3283781.S2CID35635747.
  9. ^Chasin M, Harris DN, Phillips MB, Hess SM (September 1972). "1-Ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo-(3,4-b)-pyridine-5-carboxylic acid, ethyl ester, hydrochloride (SQ 20009)--a potent new inhibitor of cyclic 3',5'-nucleotide phosphodiesterases".Biochemical Pharmacology.21(18): 2443–2450.doi:10.1016/0006-2952(72)90414-5.PMID4345859.
  10. ^Wang P, Myers JG, Wu P, Cheewatrakoolpong B, Egan RW, Billah MM (May 1997). "Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D".Biochemical and Biophysical Research Communications.234(2): 320–324.doi:10.1006/bbrc.1997.6636.PMID9177268.
  11. ^Daniel JL (2002)."Platelet signalling; cAMP and cGMP".In Gresele P (ed.).Platelets in thrombotic and non-thrombotic disorders: pathophysiology, pharmacology and therapeutics.Cambridge, UK: Cambridge University Press.ISBN0-521-80261-X.
  12. ^"EHT 0202".Pipeline.ExonHit. Archived fromthe originalon 2011-01-11.
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