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*  Palmitoylethanolamide
PEA cannot strictly be considered a classic endocannabinoid because it lacks affinity for the cannabinoid receptors CB1 and CB2 ... Phan, N. Q.; Siepmann, D.; Gralow, I.; Ständer, S. (2009). "Adjuvant topical therapy with a cannabinoid receptor agonist in ... For instance during β-amyloid-induced neuroinflammation the deregulation of cannabinoid receptors and its endogenous ligands ... O'Sullivan, S. E.; Kendall, D. A. (2010). "Cannabinoid activation of peroxisome proliferator-activated receptors: Potential for ...
*  Cannabinoid receptor type 2
Cannabinoid receptor Cannabinoid receptor type 1 (CB1) GRCh38: Ensembl release 89: ENSG00000188822 - Ensembl, May 2017 GRCm38: ... The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that ... though not as densely as the CB1 receptor and located on different cells. Unlike the CB1 receptor, in the brain, CB2 receptors ... The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1 ...
*  N-Acylamides
Anandamide activates the cannabinoid receptors CB1 and CB2. FAAH knockout mice show increased anandamide levels in vivo and ... "Opportunistic activation of TRP receptors by endogenous lipids: Exploiting lipidomics to understand TRP receptor cellular ... an orthologue of vertebrate cannabinoid receptors in the urochordate Ciona intestinalis. Gene, 302(1), 95-101. Fezza, F., ... cannabinoid-receptor dependent behaviors including antinociception and anxiolysis. GPR18, GPR55, GPR92 have also been proposed ...
*  Org 27569
... is a drug which acts as a potent and selective positive allosteric modulator of the cannabinoid CB1 receptor. Studies ... "Allosteric modulation of the cannabinoid CB1 receptor". Molecular Pharmacology. 68 (5): 1484-95. doi:10.1124/mol.105.016162. ... However while Org 27569 increases the ability of CB1 agonists to bind to the receptor, it decreases their efficacy at ... and so in practice behaves as an insurmountable antagonist of CB1 receptor function. GAT100 PSNCBAM-1 ZCZ-011 Price MR, Baillie ...
*  Drinabant
Cannabinoid receptor antagonist Lange JH, Kruse CG (2008). "Cannabinoid CB1 receptor antagonists in therapeutic and structural ... Reggio, Patricia H. (2009). "Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists". Drug ... Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ...
*  WIN 55,212-2
2012). "Sex differences in cannabinoid receptor-1 (CB1) pharmacology in mice selectively bred for high voluntary wheel-running ... WIN 55,212-2 is a full agonist at the CB1 cannabinoid receptor (Ki = 1.9 nM) and has much higher affinity than THC (Ki = 41 nM ... "Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors". Molecular Pharmacology ... "Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1". The Biochemical ...
*  LY-320,135
... a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. Journal ... LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It was ... Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sciences. 2005 Feb 4;76(12):1307-24. PMID 15670612. ... and at higher doses it also binds to a range of non-cannabinoid receptors. However LY-320,135 is still fairly widely used in ...
*  RVD-Hpα
... of cannabinoid CB1 receptors. It is shown that pepcan-12 opposite acts as a potent CB2 cannabinoid receptor positive allosteric ... which was originally proposed to act as a selective agonist for the CB1 cannabinoid receptor. It is a 12-amino acid polypeptide ... "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proceedings of the National Academy of Sciences of the United ... Recently it was shown that RVD-Hpα (also called Pepcan-12) is a potent negative allosteric modulator at CB1 receptors, together ...
*  Placebo
"Nonopioid placebo analgesia is mediated by CB1 cannabinoid receptors". Nature Medicine. 17 (10): 1228-1230. doi:10.1038/nm.2435 ...
*  Hemopressin
It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors. Longer forms of hemopressin containing 2-3 ... May 2010). "The peptide hemopressin acts through CB1 cannabinoid receptors to reduce food intake in rats and mice". J. Neurosci ... December 2007). "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proc. Natl. Acad. Sci. U.S.A. 104 (51): 20588 ... is also an agonist at CB1 cannabinoid receptors. The original Hp peptide reduces sensitivity to painful stimuli in an ...
*  GAT100
... is a negative allosteric modulator of the cannabinoid CB1 receptor. Org 27569 PSNCBAM-1 ZCZ-011 Pushkar M. Kulkarni; ... "Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, ... "Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s)". Journal of ...
*  NESS-0327
... a novel putative antagonist of the CB1 cannabinoid receptor". Journal of Pharmacology and Experimental Therapeutics. 306 (1): ... and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e ... Synthesis and Biological Activity of Rigid Cannabinoid CB1 Receptor Antagonists". Chem. Pharm. Bull. 50 (8): 1109-1113. doi: ... a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptor CB1. ...
*  Endocannabinoid enhancer
323-. ISBN 978-981-4287-59-3. Bambico, Francis Rodriguez; Gobbi, Gabriella (2008). "The cannabinoid CB1 receptor and the ... Cannabinoid receptor Synthetic cannabinoid Cannabinoid receptor antagonist George I. Papakostas; Maurizio Fava (2010). ...
*  2-Arachidonoylglycerol
January 1999). "Evidence that the cannabinoid CB1 receptor is a 2-arachidonoylglycerol receptor. Structure-activity ... 2-AG was a known chemical compound but its occurrence in mammals and its affinity for the cannabinoid receptors were first ... 2-Arachidonoylglycerol (2-AG) is an endocannabinoid, an endogenous agonist of the CB1 receptor. It is an ester formed from the ... A research group at Teikyo University reported the affinity of 2-AG for the cannabinoid receptors in 1994-1995, but the ...
*  AM-251 (drug)
AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to SR141716A (rimonabant); both ... Like SR141716A, it is additionally a μ-opioid receptor antagonist. Discovery and development of Cannabinoid Receptor 1 ... 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 ...
*  AM-694
... is an agonist for cannabinoid receptors. Affinities are: with a Ki of 0.08 nM at CB1 and 18x selectivity over CB2 with a ... Regioselective F-18 radiolabeling of AM694, a CB1 cannabinoid receptor ligand. Journal of Labelled Compounds and ... is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. It is used in scientific research for ... AM-679 AM-1235 AM-2201 AM-2232 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids THJ-2201 WO patent ...
*  Adult neurogenesis
"Cannabinoid receptor CB1 mediates baseline and activity-induced survival of new neurons in adult hippocampal neurogenesis". ... Eph receptors and ephrin signaling have been shown to regulate adult neurogenesis in the hippocampus and have been studied as ... Han, S.; Zhao, B.; Pan, X.; Song, Z.; Liu, J.; Gong, Y.; Wang, M. (2015-12-03). "Estrogen receptor variant ER-α36 is involved ... This is due to receptors in the system that can also influence the production of new neurons. Nonetheless, a study directed at ...
*  ZCZ-011
... is a positive allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 PSNCBAM-1 Justin L. Poklis; ... "A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects". ... A Novel Pharmacological Tool for Investigation of the Cannabinoid Receptor in Mouse Brain Using Clean Screen FASt™ Column ...
*  PTI-1
Indol-3-yl) heterocycle derivatives as agonists of the cannabinoid CB1 receptor. Patent US 7700634, priority date 5 March 2004 ... Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. Bioorganic & Medicinal ... PTI-1 is an indole-based synthetic cannabinoid. It is one of few synthetic cannabinoids containing a thiazole group and is ...
*  2-Arachidonyl glyceryl ether
... and Raphael Mechoulam found the endogenous agonist of the cannabinoid receptor type 1 (CB1) in 2000. The discovery was 100 gram ... 3 µM at the Cannabinoid receptor type 1 and the peripheral cannabinoid receptors. The presence of 2-AGE in body tissue is ... 2-AGE binds with a Ki of 21 nM to the CB1 receptor and 480 nM to the CB2 receptor. It shows agonistic behaviour on both ... an endogenous agonist of the cannabinoid CB1 receptor". Proceedings of the National Academy of Sciences. 98 (7): 3662-3665. doi ...
*  PSNCBAM-1
... is a negative allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 ZCZ-011 German N, Decker AM, ... a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats". British Journal of Pharmacology. ... "Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure-Activity Relationship Studies on 1-(4- ...
*  Conditioned place preference
Mice lacking the mu opioid receptor exhibited a lack of conditioned place preference. Knockouts of CB1 cannabinoid receptor ... Castane, A., Valjent, E., Ledent, C., Parmentier, M., Maldonado, R., & Valverde, O. (2002).Lack of CB1 cannabinoid receptors ... Ethanol self-administration and ethanol conditioned place pref-erence are reduced in mice lacking cannabinoid CB1 receptors. ... Studies also show a lack of conditioned place preference in CB1 receptor knockout mice, implicating a possible contribution of ...
*  Metamizole
Despite this studies in animals have found that the CB1 cannabinoid receptor is not involved in the analgesia induced by ... Elmas, P; Ulugol, A (November 2013). "Involvement of cannabinoid CB1 receptors in the antinociceptive effect of dipyrone". ... The result is a couple of cannabinoid and NSAID arachidonic acid conjugates[clarification needed] (although not in the strict ...
*  Ibipinabant
... especially structure-activity relationship studies into novel CB1 antagonists. Cannabinoid receptor antagonist Lange, JH; ... of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor ... 4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity". Bioorganic & Medicinal Chemistry ... 2007). "Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism ...
*  AM-6545
"Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity". Journal of Clinical ... AM-6545 is a drug which acts as a peripherally selective silent antagonist for the CB1 receptor, and was developed for the ... mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor ... CB-13 - a peripherally selective cannabinoid agonist O-2050 - a centrally active CB1 silent antagonist Methylnaltrexone - a ...
*  Guineesine
In addition, the analgesic and catatonic effects were reversed by the cannabinoid receptor type 1 (CB1) inverse agonist ... "Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and ... This causes an increase in the activity of the two neurotransmitters which are classified as endogenous cannabinoids. ...
*  Surinabant
Gessa, GL; Serra, S; Vacca, G; Carai, MA; Colombo, G (2005). "Suppressing effect of the cannabinoid CB1 receptor antagonist, ... Lallemand, F; De Witte, P (Jul 2006). "SR147778, a CB1 cannabinoid receptor antagonist, suppresses ethanol preference in ... Doggrell, SA (2005). "Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?". Expert ... a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization". ...