Cartazolate

Cartazolate is a topic that has captured the attention of millions of people around the world. Throughout history, it has generated great interest and intrigue, sparking debates, investigations and passionate discussions. From its origins to the present day, Cartazolate has played a crucial role in society, influencing individuals, communities and cultures in all corners of the planet. As we continue to explore and discover more about Cartazolate, its implications and its impact on the modern world, it is essential to understand its importance and implications on everyday life. In this article, we will take an in-depth look at Cartazolate, exploring its history, current relevance, and possible future, to provide a holistic view of this phenomenon.

Not to be confused with tracazolate.
Cartazolate
Clinical data
Routes of
administration		By mouth
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • Уthyl 4-(butylamino)-1-ethyl-1H-pyrazolopyridine-5-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H22N4O2
Molar mass290.367 g·mol−1
3D model (JSmol)
  • O=C(C1=CN=C(N(CC)N=C2)C2=C1NCCCC)OCC

Cartazolate (SQ-65,396) is a drug of the pyrazolopyridine class. It acts as a GABAA receptor positive allosteric modulator at the barbiturate binding site of the complex and has anxiolytic effects in animals. It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate was tested in human clinical trials and was found to be efficacious for anxiety but was never marketed. It was developed by a team at E.R. Squibb and Sons in the 1970s.

See also

References

  1. ^ Placheta P, Karobath M (March 1980). "In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes". European Journal of Pharmacology. 62 (2–3): 225–8. doi:10.1016/0014-2999(80)90281-2. PMID 6103810.
  2. ^ Supavilai P, Karobath M (March 1981). "Action of pyrazolopyridines as modulators of flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum". European Journal of Pharmacology. 70 (2): 183–93. doi:10.1016/0014-2999(81)90213-2. PMID 6114867.
  3. ^ Leeb-Lundberg F, Snowman A, Olsen RW (May 1981). "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal of Neuroscience. 1 (5): 471–7. doi:10.1523/JNEUROSCI.01-05-00471.1981. PMC 6564167. PMID 7050308.
  4. ^ Bristow DR, Martin IL (March 1990). "Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor". Journal of Neurochemistry. 54 (3): 751–61. doi:10.1111/j.1471-4159.1990.tb02315.x. PMID 2154549. S2CID 25784613.
  5. ^ Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D (February 1988). "Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655–64. doi:10.1016/0006-2952(88)90139-6. PMC 3445624. PMID 2829919.
  6. ^ Wachtel H (1982). "Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors". Psychopharmacology. 77 (4): 309–16. doi:10.1007/BF00432761. PMID 6182575. S2CID 10122417.
  7. ^ O'Brien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1.
  8. ^ US 3966746, Hoehn, Hans & Denzel, Theodor, "Amino derivatives of pyrazolopyridine carboxamides", published 1976-06-29, assigned to Squibb & Sons Inc. 
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