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Chemical Compound Review: 

SureCN10538641     9-methyl-4-phenyl-1,2,7,8...

Synonyms: LS-156694, AC1L2S2M, SR 95195, 100078-89-5
 
 
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Disease relevance of SR 95195

  • At high doses SR 95195 induced clonic seizures in mice (threshold convulsant dose: 150 mg kg-1; CD50: 160 mg kg-1 i.p.) which were antagonized by Ro 15-1788 [1].
 

High impact information on SR 95195

  • In vitro, SR 95195 displaced specifically bound [3H]-flunitrazepam from rat cerebellar and hippocampal membranes with respective IC50 values of 4 and 8 microM [1].
  • The respiratory and behavioral effects of the benzodiazepine receptor (BZR) inverse agonist ethyl-beta-carboline-3-carboxylate (beta-CCE) were determined alone and in combination with buspirone, lorazepam, flumazenil, and SR 95195 in rhesus monkeys [2].

References

  1. A 7-phenyl substituted triazolopyridazine has inverse agonist activity at the benzodiazepine receptor site. Biziere, K., Bourguignon, J.J., Chambon, J.P., Heaulme, M., Perio, A., Tebib, S., Wermuth, C.G. Br. J. Pharmacol. (1987) [Pubmed]
  2. Combination of buspirone and other drugs with beta-CCE in monkeys: effects on respiration and behavior. Wettstein, J.G., Teeple, E.S., Morse, W.H. Pharmacol. Biochem. Behav. (1993) [Pubmed]
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