Colonel William A. Phillips

U-93631 is a GABA_A receptor antagonist.

Mechanism of action

The mechanism of action of this compound is not entirely clear, but research shows that it binds to the GABA_A receptor. Its binding site seems to be similar to the one of picrotoxin, a potent neurotoxin and convulsant.

The binding of U-93631 decreases the probability of the chloride channel opening and stabilizes the receptor in an inactivated state.^[1]

References

^ Dillon, G. H.; Im, W. B.; Pregenzer, J. F.; Carter, D. B.; Hamilton, B. J. (February 1995). "[4-Dimethyl-3-t-butylcarboxyl-4,5-dihydro (1,5-a) quinoxaline] is a novel ligand to the picrotoxin site on GABAA receptors, and decreases single-channel open probability". The Journal of Pharmacology and Experimental Therapeutics. 272 (2): 597–603. ISSN 0022-3565. PMID 7531762.

[1] Dillon, G. H.; Im, W. B.; Pregenzer, J. F.; Carter, D. B.; Hamilton, B. J. (February 1995). "[4-Dimethyl-3-t-butylcarboxyl-4,5-dihydro (1,5-a) quinoxaline] is a novel ligand to the picrotoxin site on GABAA receptors, and decreases single-channel open probability". The Journal of Pharmacology and Experimental Therapeutics. 272 (2): 597–603. ISSN 0022-3565. PMID 7531762.

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