... is a classical cannabinoid derivative which acts as a potent and reasonably selective agonist for the CB1 receptor, ... a highly potent cannabinoid receptor 1 (CB1) agonist". Journal of Medicinal Chemistry. 53 (19): 6996-7010. doi:10.1021/ ... with a Ki of 0.16 nM, and 26x selectivity over the related CB2 receptor. It has high potency in animal tests of cannabinoid ... AM-906, AM-1235), as almost all commonly used CB1 agonists have similar or greater affinity for CB2 than CB1, and the only ...
... (SP-1) is an analgesic drug which acts as a potent cannabinoid receptor agonist, and was developed by Abbott ... The Cannabinoid Receptors. The Receptors. pp. 3-19. doi:10.1007/978-1-59745-503-9_1. ISBN 978-1-58829-712-9. v t e (Articles ... Cannabinoids, Benzopyrans, Propargyl compounds, Phenols, All stub articles, Cannabinoid stubs). ... A-41988 Menabitan Razdan RK (2009). "Structure-Activity Relationships of Classical Cannabinoids". In Reggio PR (ed.). ...
Mallet P, Beninger R (May 1996). "The endogenous cannabinoid receptor agonist anandamide impairs memory in rats". Behavioural ... CB1 receptor agonists, CB2 receptor agonists, Glycine receptor agonists, Glycine receptor antagonists, Euphoriants, Arachidonyl ... This metabolite of paracetamol is a potent agonist at the TRPV1 vanilloid receptor, a weak agonist at both CB1 and CB2 ... These distinct effects are mediated primarily by CB1 cannabinoid receptors in the central nervous system, and CB2 cannabinoid ...
It is a potent and reasonably selective agonist for the CB1 cannabinoid receptor, with a Ki of 1.2 nM at CB1 and 5.3 nM at CB2 ... AM-905 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is conformationally ... Papahatjis DP, Kourouli T, Abadji V, Goutopoulos A, Makriyannis A (March 1998). "Pharmacophoric requirements for cannabinoid ... AM cannabinoids, All stub articles, Cannabinoid stubs). ... affinity for and selectivity between CB1 and CB2 receptors. ...
... acts as a potent agonist for the cannabinoid receptors, with the original patent claiming approximately 4x ... is an indazole-3-carboxamide based synthetic cannabinoid. ...
They showed that cannabinoid receptor agonists, drugs that mimic the actions of endocannabinoids or THC, could evoke the same ... but by acting at a yet unknown cannabinoid receptor. Some work has shown that anandamide can bind to the vannilloid receptor ... Immunohistochemical localization of cannabinoid type 1 and vanilloid transient receptor potential vanilloid type 1 receptors in ... 1990) Cannabinoid receptor localization in brain. Proc Natl Acad Sci U S A. Mar;87(5):1932-6. Jo YH, Chen YJ, Chua SC Jr, ...
... is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, with a novel chemical structure ... a selective CB2 receptor agonist for the treatment of inflammatory pain". Journal of Medicinal Chemistry. 50 (11): 2597-2600. ... Cannabinoids, Trifluoromethyl compounds, Aminopyrimidines, Chlorobenzenes, All stub articles, Cannabinoid stubs). ... Han S, Thatte J, Jones RM (2009). Chapter 11: Recent Advances in the Discovery of CB2 Selective Agonists. Annual Reports in ...
STS-135 acts a potent cannabinoid receptor agonist in vitro, with an EC50 of 51 nM for human CB2 receptors, and 13 nM for human ... Cannabinoids, Designer drugs, Organofluorides, Indoles, Indolecarboxamides, All stub articles, Cannabinoid stubs). ... CB1 receptors. STS-135 produces bradycardia and hypothermia in rats at doses of 1-10 mg/kg, suggesting cannabinoid-like ... August 2015). "Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22 ...
JWH cannabinoids, Naphthoylindoles, CB1 receptor agonists, All stub articles, Cannabinoid stubs). ... In the United States, all CB1 receptor agonists of the 3-(1-naphthylmethane)indole class such as JWH-185 are Schedule I ... JWH-185 is a synthetic cannabinoid receptor ligand from the naphthoylindole family. It is the carbonyl-reduced derivative of ... new cannabimimetic indoles provide evidence for aromatic stacking interactions with the CB1 cannabinoid receptor". Bioorg. Med ...
JWH cannabinoids, CB1 receptor agonists, Naphthalenes, Indoles, All stub articles, Cannabinoid stubs). ... In the United States, all CB1 receptor agonists of the 3-(1-naphthylmethane)indole class such as JWH-184 are Schedule I ... JWH-184 is a synthetic cannabinoid receptor ligand from the naphthylmethylindole family. It is the carbonyl-reduced derivative ... cannabinoid receptor". Bioorganic & Medicinal Chemistry. 11 (4): 539-49. doi:10.1016/s0968-0896(02)00451-0. PMID 12538019. ...
JWH cannabinoids, Naphthoylindoles, Designer drugs, CB1 receptor agonists, All stub articles, Cannabinoid stubs). ... In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-116 are Schedule I Controlled ... JWH-116 is a synthetic cannabinoid receptor ligand from the naphthoylindole family. It is the indole 2-ethyl derivative of ... cannabinoid receptor". Bioorganic & Medicinal Chemistry. 11 (4): 539-49. doi:10.1016/s0968-0896(02)00451-0. PMID 12538019. ...
AM-679 (part of the AM cannabinoid series) is a drug that acts as a moderately potent agonist for the cannabinoid receptors, ... AM-679 was one of the first 3-(2-iodobenzoyl)indole derivatives that was found to have significant cannabinoid receptor ... and the selective CB2 agonist AM-1241. AM-679 was first identified as having been sold as a cannabinoid designer drug in ... Design and synthesis of selective cannabinoid receptor ligands: Aminoalkylindole and other heterocyclic analogs (PhD ...
Cannabinoids, CB1 receptor antagonists, All stub articles, Cannabinoid stubs). ... However while Org 27569 increases the ability of CB1 agonists to bind to the receptor, it decreases their efficacy at ... Org 27569 is a drug which acts as a potent and selective negative 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. ...
Synthetic cannabinoid receptor type 1 agonists, their salts, derivatives, isomers, and salts of derivatives and isomers - with ...
... amino acid conjugates did not have the same effects and the actions of NaGly were not affected by cannabinoid receptor agonists ... Additionally, tetrahydrocannabinol and NaGly are full agonists at the GPR18 receptors and induce migration in human endometrial ... Recently, NAGly has been found to bind to G-protein coupled receptor 18 (GPR18), the putative abnormal cannabidiol receptor. ... suggesting a novel non-cannabinoid receptor mediated approach to alleviate inflammatory pain. NaGly was shown to be endogenous ...
... synthetic cannabinoid receptor agonists and oripavine" (PDF). Archived from the original (PDF) on 2014-10-06. Retrieved 2014-03 ... GABAB receptor agonists, GHB receptor agonists, Designer drugs, GABA analogues, Drug-facilitated sexual assault). ...
Cannabinoid CB2 receptor agonists have been found to decrease the induction of ICAM-1 and VCAM-1 surface expression in human ... "Activation of cannabinoid receptor 2 attenuates leukocyte-endothelial cell interactions and blood-brain barrier dysfunction ... It binds to integrins of type CD11a / CD18, or CD11b / CD18 and is also exploited by rhinovirus as a receptor for entry into ... ICAM-1 is a ligand for LFA-1 (integrin), a receptor found on leukocytes. When activated, leukocytes bind to endothelial cells ...
... and less so for synthetic cannabinoid receptor (CBR) agonists and antagonists) and other hydrophobic molecules. Altered ... A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein". Biochemistry. 55 (37): 5243-55. doi:10.1021/acs.biochem. ... A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein". Biochemistry. 55 (37): 5243-5255. doi:10.1021/acs.biochem. ... "Fatty acids and hypolipidemic drugs regulate peroxisome proliferator-activated receptors alpha - and gamma-mediated gene ...
This compound was also tested as part of a series of cannabinoid receptor 2 agonists, and was found to be active though with ...
January 1998). "LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of ... particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. Felder CC, ... LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It was ... Pertwee RG (February 2005). "Inverse agonism and neutral antagonism at cannabinoid CB1 receptors". Life Sciences. 76 (12): 1307 ...
LCs contain a large amount of cannabinoid receptor type 2 (CB2), that by activation by agonists, attenuate both the recruitment ... Oka, Saori (2006). "Involvement of the Cannabinoid CB2 Receptor and Its Endogenous Ligand 2-Arachidonoylglycerol in Oxazolone- ... ISBN 0-443-05612-9. Hussain, LA; Lehner, T (1995). "Comparative investigation of Langerhans' cells and potential receptors for ...
... for cannabinoid receptor agonists (e.g. cannabidiol,[citation needed] dronabinol) -nabant for cannabinoid receptor antagonists ... Examples are: -anib for angiogenesis inhibitors (e.g. pazopanib) -anserin for serotonin receptor antagonists, especially 5-HT2 ... sartan for angiotensin II receptor antagonists (e.g. losartan) -tinib for tyrosine kinase inhibitors (e.g. imatinib) -vastatin ... antagonists (e.g. ritanserin and mianserin) -ant for various receptors antagonists (e.g. aticaprant and rimonabant) -arit for ...
The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced ... This results in a receptor blockade, inhibiting the binding of agonists and inverse agonists. Receptor antagonists can be ... Not every ligand that binds to a receptor also activates that receptor. The following classes of ligands exist: (Full) agonists ... The insulin receptor is an example. Type 4: Nuclear receptors - While they are called nuclear receptors, they are actually ...
... is a drug that acts as a potent but unselective agonist for the cannabinoid receptors, with a Ki of 0.28 nM at CB1 and 1.48 nM ... In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as AM-2232 are Schedule I Controlled ... AM-694 AM-1235 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids O-774 O-1057 O-1812 THJ-2201 US patent ... AM cannabinoids, Designer drugs, All stub articles, Cannabinoid stubs). ...
July 2021). "Systematic evaluation of a panel of 30 synthetic cannabinoid receptor agonists structurally related to MMB-4en- ... December 2020). "Synthesis and in Vitro Cannabinoid Receptor 1 Activity of Recently Detected Synthetic Cannabinoids 4F-MDMB- ... It was originally developed by Pfizer as a potential analgesic, and is a potent agonist of the CB1 receptor with a binding ... It is a similarly potent CB1 agonist, with a binding affinity of 0.29nM for CB1 and 0.91nM for CB2, and an EC50 of 6.36 nM for ...
April 2021). "Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists". Journal of ... AM-11245 is a drug which is a cannabinoid agonist from the classical cannabinoid family. It has high affinity and efficacy at ... making it one of the most potent cannabinoid agonists identified to date. HU-243 O-774 List of AM cannabinoids Jiang S, ... both the CB1 and CB2 cannabinoid receptors, with a Ki of 0.4nM at both CB1 and CB2, and an EC50 of ~0.06nM at CB1 and 0.2nM at ...
Cannabinoid CB2 receptor agonists are found to decrease the induction of ICAM-1 and VCAM-1 surface expression in human brain ... the cannabinoids bind to these receptors in the same way. Previous studies have shown that CB1 receptors located on the nerve ... CB1 cannabinoid receptors - which are known to be present in the brain - exist in the endothelial cells which line the gut, it ... "Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing". ...
... although this effect may be mediated through cannabinoid CB1 or CB2 receptor-independent effects. 5-HT2A receptor agonists have ... Cannabinoid type 2 receptor-dependent and -independent immunomodulatory effects". The Journal of Biological Chemistry. 281 (20 ... Several 5-HT2A agonist hallucinogens including (R)-DOI, TCB-2, LSD and LA-SS-Az have unexpectedly also been found to act as ... Nau F, Yu B, Martin D, Nichols CD (2013-10-02). "Serotonin 5-HT2A receptor activation blocks TNF-α mediated inflammation in ...
... is a drug that is a classical cannabinoid derivative, which acts as a potent agonist for cannabinoid receptors, ... US 7279500, Martin BR, Razdan RJ, Pertwee RG, "Sulfonamide Cannabinoid Agonists and Antagonists", published 5 May 2005 v t e ( ... January 2011). "Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB(1) receptor antagonist". ...
... is a drug that acts as a potent agonist for the cannabinoid receptors, with EC50 values of 2.6 nM at CB1 and 3.0 nM ... Cannabinoids, Designer drugs, Fluoroarenes, Indolecarboxamides, All stub articles, Cannabinoid stubs). ... September 2015). "Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA ...