Serotonin receptor binding affinities of several hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues

J Med Chem. 1978 Aug;21(8):822-5. doi: 10.1021/jm00206a022.

Abstract

Hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues are known to affect serotonergic systems both in vivo and in vitro. Using a rat stomach fundus model, the 5-HT receptor binding affinities of several of these analogues were determined and compared. The most behaviorally potent analogues examined, DOB, DOM, and 5-methoxy-N,N-dimethyltryptamine, were found to possess rather high affirmities (pA2 = 7.35, 7.12, and 7.08, respectively) for the 5-HT receptors of the model system.

Publication types

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

MeSH terms

  • Amines / chemical synthesis*
  • Amines / metabolism
  • Amines / pharmacology
  • Animals
  • Female
  • Hallucinogens / chemical synthesis*
  • Hallucinogens / metabolism
  • Hallucinogens / pharmacology
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • N,N-Dimethyltryptamine / analogs & derivatives
  • N,N-Dimethyltryptamine / chemical synthesis*
  • N,N-Dimethyltryptamine / metabolism
  • N,N-Dimethyltryptamine / pharmacology
  • Rats
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / metabolism*
  • Stomach / drug effects
  • Tryptamines / chemical synthesis*

Substances

  • Amines
  • Hallucinogens
  • Receptors, Serotonin
  • Tryptamines
  • N,N-Dimethyltryptamine