From Wikipedia, the free encyclopedia
Chemical compound
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.
[8]
See also
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 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .
^ O'Brien, Robert (1986).
Receptor binding in drug research . New York: Dekker. p. 519.
ISBN
0-8247-7548-1 .
^
US 3966746 , Hoehn, Hans & Denzel, Theodor, "Amino derivatives of pyrazolopyridine carboxamides", published 1976-06-29, assigned to
Squibb & Sons Inc.
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AA-29504
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Org 25,435
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