Effect of RGPU-260, a Novel GABA Derivative, on Functional Reserves of Rat Heart after Chronic Alcohol Intoxication

Bull Exp Biol Med. 2021 Mar;170(5):631-635. doi: 10.1007/s10517-021-05121-7. Epub 2021 Mar 31.

Abstract

The effect of a new derivative of GABA, the compound RGPU-260, on the heart contractility of rats exposed to chronic alcohol intoxication (10% ethanol solution for 24 weeks) was studied. In comparison with intact rats, the alcoholized ones were characterized with smaller increments in the rates of myocardial contraction (+dP/dtmax) and relaxation (-dP/dtmax), left ventricular pressure, and maximum intensity of functioning of structures during the load tests (volume load/preload, stimulation of the cardiac adrenergic receptors, and occlusion of the ascending aorta/afterload) attesting to degraded cardiac contractility function. In rats treated with RGPU-260 (daily, 25 mg/kg intragastrically during 14 days), these parameters were higher in comparison with control values indicating a positive action of the examined agent on inotropic function of the heart. Effectiveness of cardiotropic action of RGPU-260 was comparable to that of the reference drug mildronate.

Keywords: cardioprotective effects; chronic alcohol intoxication; derivatives of GABA.

MeSH terms

  • Alcoholic Intoxication / drug therapy
  • Animals
  • Cardiotonic Agents / chemistry*
  • Cardiotonic Agents / pharmacology*
  • Female
  • Heart / drug effects
  • Heart Rate / drug effects
  • Rats
  • gamma-Aminobutyric Acid / chemistry*
  • gamma-Aminobutyric Acid / pharmacology*

Substances

  • Cardiotonic Agents
  • gamma-Aminobutyric Acid