Antagonism of inhibitory amino acids by the steroid derivative RU5135.
The steroid derivative RU5135 has been tested for its ability to antagonize glycine and the gamma-aminobutyric acid (GABA) analogue muscimol on isolated preparations of rat optic nerve and cuneate nucleus, respectively. On the cuneate nucleus, RU5135 antagonized muscimol in a competitive manner with a pA2 value of 8.31. RU5135 shared a common site of action with bicuculline that was separate from the picrotoxin site. On the optic nerve, RU5135 antagonized glycine with a pA2 of 7.67. It shared a common site of action with strychnine.
D000596:Amino Acids / Q000037:antagonists & inhibitors*; D000731:Androstanes / Q000494:pharmacology*; D000818:Animals; D001378:Azasteroids / Q000494:pharmacology*; D001640:Bicuculline / Q000494:pharmacology; D004594:Electrophysiology; D005998:Glycine / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D008526:Medulla Oblongata / Q000502:physiology; D009118:Muscimol / Q000037:antagonists & inhibitors; D009900:Optic Nerve / Q000502:physiology; D010852:Picrotoxin / Q000494:pharmacology; D051381:Rats; D013260:Steroids, Heterocyclic / Q000494:pharmacology*; D013331:Strychnine / Q000494:pharmacology
D000596:Amino Acids; D000731:Androstanes; D001378:Azasteroids; D001640:Bicuculline; D005998:Glycine; D009118:Muscimol; D010852:Picrotoxin; D013260:Steroids, Heterocyclic; D013331:Strychnine; C032061:RU 5135