Structure-anticonvulsant activity relationships of cannabidiol analogs

NIDA Res Monogr. 1987:79:48-58.

Abstract

Cannabidiol (CBD) exhibits anticonvulsant activity in experimental animals and in man. As part of a structure-activity study, analogs were prepared wherein the terpene unit, the aryl unit, and/or the side chain were modified. Thus, several pinenyl and carenyl derivatives, aryl ethers and acetates, and a variety of 1",1"-dialkylhexyl and 1",1"-dialkylheptyl analogs were synthesized. The compounds were evaluated for anti-convulsant activity in seizure susceptible (AGS) rats and for neurotoxicity in the rat rotorod (ROT) test. Comparisons of stereoisomers of CBD and several analogs revealed a general lack of stereoselectivity for anticonvulsant and other CNS properties of this class of compounds.

Publication types

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

MeSH terms

  • Animals
  • Anticonvulsants*
  • Cannabidiol / analogs & derivatives
  • Cannabidiol / pharmacology*
  • Cannabinoids / pharmacology*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Rats
  • Seizures / drug therapy
  • Structure-Activity Relationship

Substances

  • Anticonvulsants
  • Cannabinoids
  • Cannabidiol