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Etazolate - Wikipedia

From Wikipedia, the free encyclopedia

Chemical compound

Pharmaceutical compound

Etazolate (SQ-20,009, EHT-0202) is an anxiolytic drug which is a pyrazolopyridine derivative and has unique pharmacological properties.[1][2][3] It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site,[4][5][6][7] as an adenosine antagonist of the A1 and A2 subtypes,[8] and as a phosphodiesterase inhibitor selective for the PDE4 isoform.[9][10][11] It is currently in clinical trials for the treatment of Alzheimer's disease.[12]

  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. 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 from the original on 2011-01-11.
Anxiolytics

(

N05B

)

5-HT1ARTooltip 5-HT1A receptor agonists GABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulators Gabapentinoids
(α2δ VDCC blockers) Antidepressants Sympatholytics
(Antiadrenergics) Others GABAA receptor positive modulators Alcohols Barbiturates Benzodiazepines Carbamates Flavonoids Imidazoles Kava constituents Monoureides Neuroactive steroids Nonbenzodiazepines Phenols Piperidinediones Pyrazolopyridines Quinazolinones Volatiles/gases Others/unsorted See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators Purine receptor modulators 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 See also: Receptor/signaling modulators

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