Phenethylamine hallucinogens in the locus coeruleus: potency of action correlates with rank order of 5-HT2 binding affinity

Eur J Pharmacol. 1986 Dec 2;132(1):79-82. doi: 10.1016/0014-2999(86)90014-2.

Abstract

The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2 binding affinity [-) DOB greater than DOM greater than ( + )DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into structure-activity relationships at 5-HT2 receptors and support earlier findings that the actions of hallucinogens displayed in the LC are mediated via 5-HT2 receptors.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amphetamines / pharmacology*
  • Animals
  • DOM 2,5-Dimethoxy-4-Methylamphetamine / analogs & derivatives
  • DOM 2,5-Dimethoxy-4-Methylamphetamine / pharmacology*
  • Dose-Response Relationship, Drug
  • Electric Stimulation
  • Evoked Potentials / drug effects
  • Isomerism
  • Locus Coeruleus / drug effects*
  • Locus Coeruleus / metabolism
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / metabolism*

Substances

  • Amphetamines
  • Receptors, Serotonin
  • DOM 2,5-Dimethoxy-4-Methylamphetamine