Cartazolate Explained

Cartazolate should not be confused with tracazolate.

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.[1] [2] [3] [4] It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor.[5] [6] Cartazolate was tested in human clinical trials and was found to be efficacious for anxiety but was never marketed.[7] It was developed by a team at E.R. Squibb and Sons in the 1970s.

See also

Notes and References

  1. Placheta P, Karobath M . 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 . March 1980 . 6103810 . 10.1016/0014-2999(80)90281-2.
  2. Supavilai P, Karobath M . Action of pyrazolopyridines as modulators of [3H]flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum . European Journal of Pharmacology . 70 . 2 . 183–93 . March 1981 . 6114867 . 10.1016/0014-2999(81)90213-2.
  3. Leeb-Lundberg F, Snowman A, Olsen RW . Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites . Journal of Neuroscience . 1 . 5 . 471–7 . May 1981 . 7050308 . 10.1523/JNEUROSCI.01-05-00471.1981. 6564167 . free .
  4. Bristow DR, Martin IL . Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor . Journal of Neurochemistry . 54 . 3 . 751–61 . March 1990 . 2154549 . 10.1111/j.1471-4159.1990.tb02315.x. 25784613 .
  5. Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D . Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors . . 37 . 4 . 655–64 . February 1988 . 2829919 . 10.1016/0006-2952(88)90139-6. 3445624.
  6. Wachtel H . Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors . Psychopharmacology . 77 . 4 . 309–16 . 1982 . 6182575 . 10.1007/BF00432761. 10122417 .
  7. Book: O'Brien, Robert . Receptor binding in drug research . Dekker . New York . 1986 . 519 . 0-8247-7548-1 .

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