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

  title={Structure of a cannabinoid receptor and functional expression of the cloned cDNA},
  author={Lisa A. Matsuda and Stephen J Lolait and Michael J. Brownstein and Alice C. Young and Tom I. Bonner},
MARIJUANA and many of its constituent cannabinoids influence the central nervous system (CNS) in a complex and dose-dependent manner1,2. Although CNS depression and analgesia are well documented effects of the cannabinoids, the mechanisms responsible for these and other cannabinoid-induced effects are not so far known3. The hydrophobic nature of these substances has suggested that cannabinoids resemble anaesthetic agents in their action, that is, they nonspecifically disrupt cellular membranes… 

Evidence for a cannabinoid receptor in immunomodulation by cannabinoid compounds.

  • N. Kaminski
  • Biology
    Advances in experimental medicine and biology
  • 1993
The objective of the presently reported studies was to explore the possibility that immune inhibition by cannabimimetic agents is mediated through a cannabinoid receptor present on immunocytes.

Molecular neurobiology of the cannabinoid receptor.

Cannabinoid Receptors and Their Endogenous Agonist, Anandamide

This review discusses recent progress in cannabinoid research with a focus on the receptors for Δ9-THC, their coupling to second messenger responses, and the endogenous lipid cannabimimetic, anandamide.

Cannabinoid receptors and their endogenous ligands.

Results of structure-activity relationship experiments revealed that 2-arachidonoylglycerol, but not anandamide, is the intrinsic natural ligand for the cannabinoid receptor.

The neurobiology and evolution of cannabinoid signalling.

  • M. ElphickM. Egertová
  • Biology
    Philosophical transactions of the Royal Society of London. Series B, Biological sciences
  • 2001
A model of cannabinoid signalling is presented in which anandamide is synthesized by postsynaptic cells and acts as a retrograde messenger molecule to modulate neurotransmitter release from presynaptic terminals, concluding that the cannabinoid signalling system may be quite restricted in its phylogenetic distribution.

Lovinger Evidence for novel cannabinoid receptors

The case for these additional receptors implicated in the endothelium-dependent vasodilator effect of certain cannabinoids and in the presynaptic inhibition of glutamatergic neurotransmission in the hippocampus are being reviewed here.

Biosynthesis and cannabinoid receptor affinity of the novel eicosanoid, conjugated triene anandamide.

The interest is focused in the screening of natural product extracts from marine organisms for agents that bind with high affinity to the cannabinoid receptor, and the use of the unusual fatty acid metabolizing systems of marine algae to make correspondingly unique analogs of anandamide.

Evidence for novel cannabinoid receptors.

Cannabinoid receptors and their endogenous agonists.

Progress is being made in the development of novel agonists and antagonists with receptor subtype selectivity, mice with genetic deletion of the cannabinoid receptors, and receptor-specific antibodies, which should help in providing a better understanding of the physiological role of the cannabinoids.

Cannabinoids and the Brain

The cannabinoid system in the brain is targetted in the use and abuse of preparations from the Cannabis plant, whose primary target in the central nervous system is the CB1 cannabinoid receptor, a G protein-coupled receptor expressed to unusually high levels.



Cannabinoid Receptors and Modulation of Cyclic AMP Accumulation in the Rat Brain

The modulation of cyclic AMP accumulation by desacetyllevonantradol could be attenuated following stereotaxic implantation of pertussis toxin, supporting the involvement of a G protein in the cannabinoid response in the brain.

Effects of the cannabinoids on physical properties of brain membranes and phospholipid vesicles: fluorescence studies.

Findings indicate that the psychoactive cannabinoids increase fluidity in the hydrophobic core of brain membranes and support a membrane perturbant hypothesis of the mechanism of delta 9-THC action.

cDNA eloping of bovine substance-K receptor through oocyte expression system

The result provides the first indication that the neuropeptide receptor has sequence similarity with rhodopsin-type receptors (the G-protein-coupled receptor family) and thus possesses multiple membrane-spanning domains.

Lutropin-choriogonadotropin receptor: an unusual member of the G protein-coupled receptor family.

The LH-CG-R gene may have evolved by recombination of LRG and G protein-coupled receptor genes and bind human choriogonadotropin with high affinity and show an increase in cyclic adenosine monophosphate when exposed to hormone.

Identification of a family of muscarinic acetylcholine receptor genes.

Analysis of human and rat genomic clones indicates that there are at least four functional muscarinic receptor genes and that these genes lack introns in the coding sequence.

Mesencephalic dopamine neurons regulate the expression of neuropeptide mRNAs in the rat forebrain.

We used in situ hybridization histochemistry with synthetic oligodeoxyribonucleotide probes to identify cells that synthesize mRNAs encoding tyrosine hydroxylase in the mesencephalon and substance P,

Cloning and sequencing of porcine LH-hCG receptor cDNA: variants lacking transmembrane domain.

Hydropathy analysis suggests the existence of seven transmembrane domains that show homology with the corresponding regions of other G protein-coupled receptors.