Cannabinoid Receptor Localization in Brain: Relationship to Motor and Reward Systems

  title={Cannabinoid Receptor Localization in Brain: Relationship to Motor and Reward Systems},
  author={Miles Herkenham},
  journal={Annals of the New York Academy of Sciences},
  • M. Herkenham
  • Published 1 June 1992
  • Biology
  • Annals of the New York Academy of Sciences
Marijuana (Omnabri satipa) is one of the oldest and most widely used drugs in the world, with a history of use dating back over 4,000 years.l.2 It was not until about twenty years ago that the principal psychoactive ingredient of the marijuana plant was isolated and found to be A9-tetrahydrocannabinol (A9-THC).3-5 A9-THC and other natural and synthetic cannabinoids produce characteristic behavioral and cognitive effect^,^.^ most of which can be attributed to actions on the central nervous… 

Cannabinoids on the Brain

Advances in understanding of the actions of cannabinoids and the brain endocannabinoid system have led to important new insights into neuronal function which are likely to result in the development of new therapeutic strategies for the treatment of a number of key CNS disorders.

Neuroanatomical basis for therapeutic applications of cannabinoid receptor 1 antagonists

The ongoing elucidation and characterization of the neuroanatomical circuitry within which the CB1 cannabinoid receptor and endocannabinoids are localized to modulate these psychological and physiological processes continues to suggest therapeutic applications for cannabinoid antagonists and inverse agonists.

Endocannabinoids and striatal function: implications for addiction-related behaviours

Recent findings in rodents showing selective pharmacological modulation of impulsivity and anxiety by cannabinoid agents are integrated and discussed and the potential of selective inhibitors of endocannabinoid metabolism, directed at fatty acid amide hydrolase and monoacylglycerol lipase, to reduce anxiety and stress responses is highlighted.

The Medical Effects Of Marijuana On the Brain New research on marijuana confirms that it damages cognitive functioning

The ramifications of some of the most important scientific discoveries about marijuana and its negative impact on the brain are analyzed.


The ability of cannabinoid medicines to treat pain, associated sleep disorders, appetite loss, muscle spasm and a wide variety of other symptoms suggests that such agents may in the future play an important role in palliative care.

The roles of cannabinoid CB1 and CB2 receptors in cocaine-induced behavioral sensitization and conditioned place preference in mice

CB 1 R and CB 2 R have opposite roles in modulating cocaine-induced sensitization and CPP, possibly by preventing neuronal activation in the hippocampus.

Cannabinoid receptor gene (CNR1): association with IV drug use

The results are consistent with a role of cannabinoid receptors in the modulation of dopamine and cannabinoid reward pathways and the association with specific types of drug dependence was greatest for cocaine, amphetamine, and cannabis dependence.

Current evidence supporting a role of cannabinoid CB1 receptor (CB1R) antagonists as potential pharmacotherapies for drug abuse disorders

This report critically reviews preclinical and clinical studies involving the ability of CB1R antagonists to attenuate the effects of drugs of abuse, while providing an overview of the neuroanatomical and neurochemical points of contact between the endocannabinoid system and systems mediating abuse-related effects.



Structure of a cannabinoid receptor and functional expression of the cloned cDNA

The cloning and expression of a complementary DNA that encodes a G protein-coupled receptor that is involved in cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana are suggested.

Cannabinoid receptor localization in brain.

  • M. HerkenhamA. Lynn K. Rice
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences of the United States of America
  • 1990
The potencies of a series of natural and synthetic cannabinoids as competitors of [3H]CP 55,940 binding correlated closely with their relative potencies in several biological assays, suggesting that the receptor characterized in the in vitro assay is the same receptor that mediates behavioral and pharmacological effects of cannabinoids, including human subjective experience.

Cellular effects of cannabinoids.

The many studies that have been included in this review suggest that cannabinoids have ubiquitous effects on biological systems and that low doses of delta 9-THC are capable of producing the psychoactivity that is unique to cannabinoids, whereas higher doses may produce effects that are both specific and nonspecific for cannabinoids.

Delta 9-tetrahydrocannabinol increases arachidonic acid levels in guinea pig cerebral cortex slices.

In brain, as in extra-neural cells in culture, cannabinoids increase unesterified AA levels; however, the relative potencies of the cannabinoids the authors examined in increasing AA levels do not correlate well with their in vivo psychoactive potencies.

Pharmacology and stereoselectivity of structurally novel cannabinoids in mice.

The pharmacological effects of three stereoisomeric pairs of structurally novel cannabinoids were tested after i.v. administration in mice for depression of spontaneous activity and the production of hypothermia, antinociception and catalepsy to demonstrate the high degree of enantioselectivity and potency.

Nonclassical cannabinoid analgetics inhibit adenylate cyclase: development of a cannabinoid receptor model.

It is postulated that the receptor that is associated with the regulation of adenylate cyclase in vitro may be the same receptor as that mediating analgesia in vivo, and a conceptualization of the cannabinoid analgetic receptor is presented.

Determination and characterization of a cannabinoid receptor in rat brain.

The criteria for a high affinity, stereoselective, pharmacologically distinct cannabinoid receptor in brain tissue have been fulfilled.

Drugs abused by humans preferentially increase synaptic dopamine concentrations in the mesolimbic system of freely moving rats.

  • G. Di ChiaraA. Imperato
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 1988
The effect of various drugs on the extracellular concentration of dopamine in two terminal dopaminergic areas, the nucleus accumbens septi (a limbic area) and the dorsal caudate nucleus (a

Characterization and localization of cannabinoid receptors in rat brain: a quantitative in vitro autoradiographic study

The results suggest that the presently characterized cannabinoid receptor mediates physiological and behavioral effects of natural and synthetic cannabinoids, because it is strongly coupled to guanine nucleotide regulatory proteins and is discretely localized to cortical, basal ganglia, and cerebellar structures involved with cognition and movement.