Etazolate

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]

Etazolate
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H19N5O2
Molar mass289.339 g·mol−1
3D model (JSmol)

Synthesis
Cartazolate and Etazolate synthesis: E.R. SQUIBB & SONS, INC., NEW YORK, N.Y., US. DE 2123318
gollark: How would you just get an "evil" version anyway? No (long-lived) empire really just sets out and goes "let's be evil" surely?
gollark: Someone asked this somewhere, I'm sure…
gollark: The trouble with brains is that if you stick them into full-power-off (no oxygen supply or whatever) they can't really turn back on again, unlike (sane) computer systems.
gollark: From my limited trek knowledge they just sit there doing nothing.
gollark: Little-to-no material scarcity doesn't mean there's not anything people want which isn't free.A relevant question is why lots of jobs shown in some of the nanofics aren't done by nonsophont AIs, though.

See also

References
  1. Hall, Judith A.; Morton, Ian (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): 619–28. 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): 833–41. 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): 207–14. doi:10.1016/0014-2999(96)00066-0. PMID 8773466.
  5. Remington, Gary; Baskys, Andrius (1996). Brain mechanisms and psychotropic drugs. Boca Raton: CRC Press. ISBN 0-8493-8386-2.
  6. M. Mishina; Kurachi, Yoshihisa (2000). Pharmacology of ionic channel function: activators and inhibitors. Berlin: Springer. ISBN 3-540-66127-1.
  7. Progress in Drug Research / Volume 31 (Progress in Drug Research). Boston: Birkhauser. 1987. 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): 433–41. doi:10.1016/0091-3057(88)90182-7. PMID 3283781.
  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): 2443–50. 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): 320–4. doi:10.1006/bbrc.1997.6636. PMID 9177268.
  11. Gresele, Paolo; Gresele, P. (2002). Platelets in thrombotic and non-thrombotic disorders: pathophysiology, pharmacology and therapeutics. Cambridge, UK: Cambridge University Press. ISBN 0-521-80261-X.
  12. "Pipeline | ExonHit". Archived from the original on 2011-01-11. Retrieved August 2010. Check date values in: |accessdate= (help)
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