• At present, there are five recognized cannabinoids produced endogenously throughout the body: Arachidonoylethanolamine (anandamide), 2-arachidonoyl glycerol (2-AG), 2-arachidonyl glyceryl ether (noladin ether), virodhamine, as well as the recently discovered N-arachidonoyl-dopamine (NADA). (wikipedia.org)
  • The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the immune system. (wikipedia.org)
  • Initial investigation of CB2 receptor expression patterns focused on the presence of CB2 receptors in the peripheral tissues of the immune system and found CB2 receptor mRNA is found throughout tissues of the spleen, tonsils, and thymus gland. (wikipedia.org)
  • of the body's cannbinoid receptors - something done naturally by cannabis and cannabinoids - may be an effective treatment and prevention strategy for itching, according to a study published in this month's issue of the journal Pharmacology , and published online by the National Institute of Health . (thejointblog.com)
  • JWH-057 - a 1-deoxy analog of Δ8-THC that has very high affinity for the CB2 receptor, but also has high affinity for the CB1 receptor. (wikipedia.org)
  • Its binding affinity at the CB1 receptor is only 51nM, making it slightly less potent than THC itself. (wikipedia.org)
  • Its binding affinity at the CB1 receptor is 42nM, around the same as that of THC, but interestingly, its analgesic potency in vivo was higher than that of other analogues with stronger CB1 binding affinity in vitro, around 3 times that of THC but with less sedative effect, most likely reflecting favorable pharmacokinetic characteristics. (wikipedia.org)
  • The resulting compound exhibits slightly better binding affinity for the CB1 receptor (with a Ki value of 7.5nM) than SR141716A, which has a Ki value of 11.5nM, AM-251 is, however, about two-fold more selective for the CB1 receptor when compared to SR141716A. (wikipedia.org)
  • These interactions induce a conformational change in the receptor structure, which triggers the activation of various intracellular signaling pathways. (wikipedia.org)
  • Activation of cannabinoid receptors could be a new therapeutic approach for the treatment of skin tumors. (greenmedinfo.com)
  • We show that anxiolysis depends on intact cannabinoid receptor 1 (CB1) receptors on forebrain GABAergic neurons and pain reduction on activation of peripheral CB1 and CB2 receptors. (pnas.org)
  • For instance, in the liver, activation of the CB1 receptor is known to increase de novo lipogenesis. (wikipedia.org)
  • This cannabinoid also prevented Aβ-induced microglial activation in vivo, and counteracted Aβ-induced reductions in the neuronal proteins calbindin and α-tubulin, the authors report. (alzforum.org)
  • Cannabinoid activation of ICRs can result in desensitization of the TRPA1 and TRPV1 channel activities, inhibition of nociceptors and antihyperalgesia and antinociception in certain pain models. (nih.gov)
  • Cannabinoids desensitize TRPV1 via activation of calcineurin and dephosphorylation of the ion channel. (nih.gov)
  • Cannabinoids desensitize TRPA1 via activation of a calcium-independent pathway. (nih.gov)
  • a) Hypothesis 1 proposes that cannabinoids produce peripheral antihyperalgesia by activation of both MCRs and ICRs. (nih.gov)
  • c) Hypothesis 3 proposes that the net effect of cannabinoids on modulating nociception is due to activation of MCRs and/or ICRs located on multiple cell types that are capable of interacting. (nih.gov)
  • GPR55 is coupled to the G-protein G13 and activation of the receptor leads to stimulation of rhoA, cdc42 and rac1. (wikipedia.org)
  • Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. (wikipedia.org)
  • Abnormal cannabidiol (Abn-CBD) is a synthetic regioisomer of cannabidiol, which unlike most other cannabinoids produces vasodilator effects, lowers blood pressure, and induces cell migration, cell proliferation and mitogen-activated protein kinase activation in microglia, but without producing any psychoactive effects. (wikipedia.org)
  • There is considerable interest in the possible therapeutic uses of marijuana and its constituent cannabinoid compounds. (eurekalert.org)
  • Cannabinoids can produce very different outcomes, depending on how they bind to the CB1 receptor," said NIDA Director Nora D. Volkow, M.D. "Understanding how these chemicals bind to the CB1 receptor will help guide the design of new medications and provide insight into the therapeutic promise of the body's cannabinoid system. (eurekalert.org)
  • Cannabinoids represent a promising class of compounds for developing novel therapeutic agents. (springer.com)
  • 2006. Cannabinoid receptors as therapeutic targets for obesity and metabolic diseases. (springer.com)
  • 2007. Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: Safety, tolerability, and therapeutic potential. (springer.com)
  • Cortical type 2 cannabinoid (CB2) receptors might serve as potential therapeutic targets for cerebral ischemia suggests a new study published in the March issue of The American Journal of Pathology . (medindia.net)
  • Evidence accumulated during the last few years suggests that GPR55 plays a relevant role in cancer and opens the possibility of considering this orphan receptor as a new therapeutic target and potential biomarker in oncology. (wikipedia.org)
  • Research of the effects on abnormal cannabidiol in mice has indicated that atypical cannabinoids have therapeutic potential in a variety of inflammatory conditions, including those of the gastrointestinal tract. (wikipedia.org)
  • Naassila M, Pierrefiche O, Ledent C, Daoust M (2004) Decreased alcohol self-administration and increased alcohol sensitivity and withdrawal in CB1 receptor knockout mice. (springer.com)
  • Defective adult neurogenesis in CB1 cannabinoid receptor knockout mice. (nih.gov)
  • GPR55 is indeed activated by endogenous, plant and synthetic cannabinoids but GPR-55 knockout mice generated by a research group from Glaxo Smith Kline showed no altered blood pressure regulation after administration of the cannabidiol-derivative abnormal cannabidiol. (wikipedia.org)
  • Sedation, in contrast, was not influenced by cannabinoid or opioid receptor blockage, and euphoria cannot be studied in mouse models. (pnas.org)
  • Lallemand F, Soubrié PH, De Witte PH (2001) Effects of CB1 cannabinoid receptor blockade on ethanol preference after chronic ethanol administration. (springer.com)
  • Despite the lack of crystal structures for CB1, protein-based homology modeling approaches and molecular docking methods can be used in the design and discovery of cannabinoid analogues. (springer.com)
  • Efficient synthetic approaches for therapeutically interesting cannabinoid analogues have been developed to further facilitate the drug discovery process. (springer.com)
  • The CB2 receptor is expressed mainly in the immune system and in hematopoietic cells. (wikipedia.org)
  • CB2 receptors are mainly expressed on T cells of the immune system, on macrophages and B cells, and in hematopoietic cells. (wikipedia.org)
  • CB2 receptors are more common in the peripheral nervous system and are linked to the immune system and pain response. (osa-opn.org)
  • Initial investigation of CB2 receptor expression patterns focused on the presence of CB2 receptors in the peripheral tissues of the immune system and found CB2 receptor mRNA is found throughout tissues of the spleen, tonsils, and thymus gland. (wikipedia.org)
  • The CB1 receptor is a pre-synaptic heteroreceptor that modulates neurotransmitter release when activated in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. (wikipedia.org)