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Cartazolate

Chemical compound

Chemical compound

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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.

References

References

  1. (March 1980). "In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes". European Journal of Pharmacology.
  2. (March 1981). "Action of pyrazolopyridines as modulators of [3H]flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum". European Journal of Pharmacology.
  3. (May 1981). "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal of Neuroscience.
  4. (March 1990). "Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor". Journal of Neurochemistry.
  5. (February 1988). "Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors". [[Biochemical Pharmacology (journal).
  6. Wachtel H. (1982). "Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors". Psychopharmacology.
  7. O'Brien, Robert. (1986). "Receptor binding in drug research". Dekker.
  8. "Amino derivatives of pyrazolopyridine carboxamides".
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adenosine-receptor-antagonists secondary-amines ethyl-esters carboxylate-esters gabaa-receptor-positive-allosteric-modulators phosphodiesterase-inhibitors pyrazolopyridines butyl-compounds
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