Potent anorexic-like effects of RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane) in the rat: a comparison with other dopamine-receptor agonists

Neuropharmacology. 1982 Sep;21(9):885-90. doi: 10.1016/0028-3908(82)90080-6.

Abstract

Modification of food intake and motor activity was investigated following administration of amphetamine (AMP), apomorphine (APO) and three novel 2-aminoindanes (2-AI): 2-di-n-propylaminoindane (JPC-60-36), 2-di-n-propylamino-5,6-dimethoxyindane (JPC-211) and 2-di-n-propylamine-4,7-dimethoxyindane (RDS-127). These compounds demonstrated dose- and time-related inhibition of food intake in male rats which were habituated to eating 4 hr each day. The ranked potencies were as follows: RDS-127 greater than AMP = APO greater than JPC-60-36 and JPC-211 was inactive. 2-di-n-Propylamine-4,7-dimethoxyindane (RDS-127) did not increase motor activity in a dose range that Significantly inhibited food intake (66% of control intake with 0.08 mumol/kg). Food intake inhibition was blocked by pimozide, but not by propranolol or phentolamine. The anorectic-like actions of RDS-127 were long-lasting (greater than 4 hr) and RDS-127 was approximately 3-fold more potent than amphetamine or apomorphine in producing increased locomotor activity; the other 2-aminoindanes were less potent in producing hyperactivity. Hyperactivity responses were blocked by pimozide, but not by alpha-methyl-p-tyrosine. These results suggest that 2-aminoindanes may modify motor behaviors, at least in part, via direct stimulation of dopamine receptors. The structure-activity relationships of 2-aminoindanes on locomotor activity and inhibition of food intake are discussed.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Anorexia / physiopathology
  • Apomorphine / pharmacology*
  • Dextroamphetamine / pharmacology*
  • Energy Intake
  • Feeding Behavior / drug effects*
  • Indans / pharmacology*
  • Indenes / pharmacology*
  • Kinetics
  • Male
  • Motor Activity / drug effects
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / drug effects
  • Receptors, Dopamine / physiology*

Substances

  • Indans
  • Indenes
  • Receptors, Dopamine
  • 2-di-n-propylaminoindan
  • 2-N,N-di-n-propylamino-4,7-dimethoxyindan
  • Apomorphine
  • Dextroamphetamine