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Etazolate

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
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 mass289.339 g·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 ananxiolyticdrug which is apyrazolopyridinederivative and has uniquepharmacological properties.[1][2][3] It acts as apositive allosteric modulator of theGABAA receptor at thebarbituratebinding site,[4][5][6][7] as anadenosineantagonist of theA1 andA2 subtypes,[8] and as aphosphodiesterase inhibitor selective for thePDE4isoform.[9][10][11] It is currently inclinical trials for the treatment ofAlzheimer's disease.[12]

See also

[edit]

References

[edit]
  1. ^Hall JA, Morton I (1999).Concise dictionary of pharmacological agents: properties and synonyms. Kluwer Academic.ISBN 0-7514-0499-3.
  2. ^Williams M (May 1983). "Anxioselective anxiolytics".Journal of Medicinal Chemistry.26 (5):619–628.doi:10.1021/jm00359a001.PMID 6132997.
  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.PMID 449623.
  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.PMID 8773466.
  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.ISBN 0-8493-8386-2.
  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.ISBN 3-540-66127-1.
  7. ^Olsen RW (1987)."GABA-Drug Interactions". In Jucker E (ed.).Progress in Drug Research. Vol. 31. Boston: Birkhauser. p. 526.ISBN 3-7643-1837-6.
  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.PMID 3283781.S2CID 35635747.
  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.PMID 4345859.
  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.Bibcode:1997BBRC..234..320W.doi:10.1006/bbrc.1997.6636.PMID 9177268.
  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.ISBN 0-521-80261-X.
  12. ^"EHT 0202".Pipeline. ExonHit. Archived fromthe original on 2011-01-11.
5-HT1ARTooltip 5-HT1A receptoragonists
GABAARTooltip GABAA receptorPAMsTooltip positive allosteric modulators
Gabapentinoids
(α2δVDCCblockers)
Antidepressants
Sympatholytics
(Antiadrenergics)
Others
Alcohols
Barbiturates
Benzodiazepines
Carbamates
Flavonoids
Imidazoles
Kava constituents
Monoureides
Neuroactive steroids
Nonbenzodiazepines
Phenols
Piperidinediones
Pyrazolopyridines
Quinazolinones
Volatiles/gases
Others/unsorted
Receptor
(ligands)
P0 (adenine)
P1
(adenosine)
P2
(nucleotide)
P2X
(ATPTooltip Adenosine triphosphate)
P2Y
Transporter
(blockers)
CNTsTooltip Concentrative nucleoside transporters
ENTsTooltip Equilibrative nucleoside transporters
PMATTooltip Plasma membrane monoamine transporter
Enzyme
(inhibitors)
XOTooltip Xanthine oxidase
Others
Others
PDE1
PDE2
PDE3
PDE4
PDE5
PDE7
PDE9
PDE10
PDE11
Non-selective
Unsorted
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