Agonistic Properties of Cannabidiol at 5-HT1a Receptors

  title={Agonistic Properties of Cannabidiol at 5-HT1a Receptors},
  author={Ethan B Russo and Andrea Burnett and Brian Hall and Keith K. Parker},
  journal={Neurochemical Research},
Cannabidiol (CBD) is a major, biologically active, but psycho-inactive component of cannabis. In this cell culture-based report, CBD is shown to displace the agonist, [3H]8-OH-DPAT from the cloned human 5-HT1a receptor in a concentration-dependent manner. In contrast, the major psychoactive component of cannabis, tetrahydrocannabinol (THC) does not displace agonist from the receptor in the same micromolar concentration range. In signal transduction studies, CBD acts as an agonist at the human 5… 

Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB2 Receptors

It is confirmed that CBD does not bind with high affinity to the orthosteric site of the human CB2R where the synthetic cannabinoid, [3H]-WIN 55,212-2, binds, and CBD was, however, able to produce minor but consistent reduction in the homogeneous binding assays in living cells using the fluorophore-conjugatedCB2R-selective compound, CM-157.

Cannabidiol inhibits the hyperphagia induced by cannabinoid-1 or serotonin-1A receptor agonists

Potential antipsychotic properties of central cannabinoid (CB1) receptor antagonists

  • P. RoserF. VollenweiderW. Kawohl
  • Psychology, Biology
    The world journal of biological psychiatry : the official journal of the World Federation of Societies of Biological Psychiatry
  • 2010
Preclinical and clinical studies investigating the potential antipsychotic effects of both CBD and SR141716 are presented together with the possible underlying mechanisms of action.

Cannabidiol Acts at 5-HT1A Receptors in the Human Brain: Relevance for Treating Temporal Lobe Epilepsy

Evaluated cell membranes show that CBD interacts with human 5-HT1A receptors of the hippocampus and temporal neocortex, and at low concentrations, the effect of CBD upon Gi/o protein activation is limited, however, at high concentrations, CBD acts as an inverse agonist of 5- HT1A receptor.

The Nonpsychoactive Cannabinoid Cannabidiol Inhibits 5-Hydroxytryptamine3A Receptor-Mediated Currents in Xenopus laevis Oocytes

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Hallucinogens and serotonergic mechanisms.

Using [3H]DOB as radioligand to minimize differences observed between agonists and antagonists, 5-HT2 affinity is related both to the lipophilicity and electron withdrawing nature of the 4-position substituents.

Comparative receptor binding analyses of cannabinoid agonists and antagonists.

The results suggest that CP-55,940, WIN55212-2 and other agonists interact with cannabinoid binding sites within the brain which are distinguishable from the population of binding sites for SR141716A, its analogs and cannabidiol.

Modulation of cannabinoid agonist binding by 5‐HT in the rat cerebellum

A membrane‐delimited cross‐talk between two G protein‐coupled receptors that are co‐localized in certain cells of the central nervous system is supported, and the cannabinoid agonist dependence of the 5‐HT modulatory effect suggests that agonist‐specific conformations of the CB1 receptor may also be important in determining the extent of this cross‐ talk.

International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors

It is considered premature to rename cannabinoid receptors after an endogenous agonist as is recommended by the International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification, because pharmacological evidence for the existence of additional types of cannabinoid receptor is emerging and other kinds of supporting evidence are still lacking.

Cannabidiol and (-)Delta9-tetrahydrocannabinol are neuroprotective antioxidants.

Cannabidiol was more protective against glutamate neurotoxicity than either ascorbate or alpha-tocopherol, indicating it to be a potent antioxidant, and data suggest that the naturally occurring, nonpsychotropic cannabinoid, cannABidiol, may be a potentially useful therapeutic agent for the treatment of oxidative neurological disorders such as cerebral ischemia.

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  • R. Pertwee
  • Biology, Medicine
    Pharmacology & therapeutics
  • 1997

Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide.

An interesting set of analogs was identified that inhibit rather than potentiate the 5-HT2A, but not the5-HT1A, receptor response, further suggesting that such analogs may permit the selective modulation of serotonin receptor subtypes and even have opposing effects on the different subtypes.

Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide

Results suggest that VR1 receptors, or increased levels of endogenous AEA, might mediate some of the pharmacological effects of CBD and its analogues, and (−)‐5′‐DMH‐CBD represents a valuable candidate for further investigation as inhibitor of AEA uptake and a possible new therapeutic agent.