From Wikipedia, the free encyclopedia
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]
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[edit] References
- ^ 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.
- ^ Supavilai P, Karobath M (March 1981). "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. doi:10.1016/0014-2999(81)90213-2. PMID 6114867. http://linkinghub.elsevier.com/retrieve/pii/0014-2999(81)90213-2.
- ^ 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. PMID 7050308. http://www.jneurosci.org/cgi/pmidlookup?view=long&pmid=7050308.
- ^ 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. PMID 2154549.
- ^ 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. PMID 2829919.
- ^ 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.
- ^ O'Brien, Robert (1986). Receptor binding in drug research. New York: Dekker. pp. 519. ISBN 0-8247-7548-1. http://books.google.com/books?id=GDE2VTeeHPIC&lpg=PA78&dq=cartazolate&pg=PA78#v=onepage&q&f=false.
