AMG-3
... is a potent agonist at both CB1 and CB2 receptors with a Ki of 0.32nM at CB1 and 0.52nM at CB2, and its particularly high ... "Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'". Journal of ... AMG-3 (part of the AM cannabinoid series) is an analgesic drug which is a cannabinoid agonist. It is a derivative of Δ8THC ... Papahatjis DP, Kourouli T, Abadji V, Goutopoulos A, Makriyannis A (March 1998). "Pharmacophoric requirements for cannabinoid ...
CUMYL-PINACA
... having an EC50 of 0.15nM for human CB1 receptors and 0.41nM for human CB2 receptors. In its pure form, it is described as a ... CUMYL-PINACA acts as a potent agonist for the cannabinoid receptors, with approximately 3x selectivity for CB1, ... Cannabinoids, Designer drugs, Indazolecarboxamides, All stub articles, Cannabinoid stubs). ... Dobaja M, Grenc D, Kozelj G, Brvar M (March 2017). "Occupational transdermal poisoning with synthetic cannabinoid cumyl-PINACA ...
O-2372
It has high affinity for both CB1 and CB2 receptors, with Ki values of 1.3 nM at CB1 and 0.57 nM at CB2, but is only moderately ... O-2372 is an analgesic cannabinoid derivative created by Organix Inc. for use in scientific research. ... "Pharmacological characterization of novel water-soluble cannabinoids". The Journal of Pharmacology and Experimental ...
AM-679 (cannabinoid)
AM-679 (part of the AM cannabinoid series) is a drug that acts as a moderately potent agonist for the cannabinoid receptors, ... and the selective CB2 agonist AM-1241. AM-679 was first identified as having been sold as a cannabinoid designer drug in ... AM-679 was one of the first 3-(2-iodobenzoyl)indole derivatives that was found to have significant cannabinoid receptor ... Design and synthesis of selective cannabinoid receptor ligands: Aminoalkylindole and other heterocyclic analogs (PhD ...
Perrottetinene
In 2018, a study showed that perrottetinene is mild to moderately psychoactive through activation of the cannabinoid receptor 1 ... cis-PET was found to have a binding affinity of 481nM at CB1 and 225nM at CB2 while the unnatural (-)-trans-PET was found to ... Cannabinoids, Benzochromenes, Phenols, All stub articles, Cannabinoid stubs). ... Perrottetinene is a naturally occurring cannabinoid compound found in liverworts from the genus Radula native to Japan, New ...
O-1602
... does not bind to the classical cannabinoid receptors CB1 or CB2 with any significant affinity, but instead is an agonist ... These previously orphan receptors have been found to be targets for a number of endogenous and synthetic cannabinoid compounds ... at several other receptors which appear to be related to the cannabinoid receptors, particularly GPR18 and GPR55. ... non-CB2 mediated effects that have become evident in the course of cannabinoid research. O-1602 produces some effects shared ...
AB-CHMINACA
... is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor (Ki = 0.78 nM) and CB2 ... November 2020). "in Vitro Cannabinoid Receptor 1 Activity of Recently Detected Synthetic Cannabinoids 4F-MDMB-BICA, 5F-MPP-PICA ... Continuing the trend seen in other cannabinoids of this generation, such as AB-FUBINACA and AB-PINACA, it contains a valine ... Trecki J, Gerona RR, Schwartz MD (July 2015). "Synthetic Cannabinoid-Related Illnesses and Deaths". The New England Journal of ...
AM-11245
It has high affinity and efficacy at both the CB1 and CB2 cannabinoid receptors, with a Ki of 0.4nM at both CB1 and CB2, and an ... 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. ... making it one of the most potent cannabinoid agonists identified to date. HU-243 O-774 List of AM cannabinoids Jiang S, ...
AM-2389
... and 26x selectivity over the related CB2 receptor. It has high potency in animal tests of cannabinoid activity, and a medium ... AM-2389 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/ ... but only the cyclobutyl derivatives show selectivity for CB1 over CB2. High selectivity for CB1 over CB2 is difficult to ...
O-1057
... which gives it considerable advantages over many related cannabinoids. It has moderate affinity for both CB1 and CB2 receptors ... a potent water-soluble cannabinoid receptor agonist with antinociceptive properties". British Journal of Pharmacology. 129 (8 ... Cannabinoid stubs, Cannabinoids, Benzochromenes, Carboxylate esters, 4-Morpholinyl compounds, Nitriles). ... O-1057 is an analgesic cannabinoid derivative created by Organix Inc., Newburyport, Massachusetts, for use in scientific ...
Naphthoylindoles
... can bind to endocannabinoid receptors in animals, presenting as CB1 and/or CB2 partial/full agonists. They ... "Synthetic cannabinoids drug profile". emcdda.europa.eu. EMCDDA. Retrieved 21 May 2023. (All stub articles, Cannabis stubs, ... v t e Naphthoylindoles are a class of synthetic cannabinoids. Behaving similarly in vivo to endocannabinoids such as anandamide ... Structural scheduling of synthetic cannabinoids Manera C, Tuccinardi T, Martinelli A (2008). "Indoles and related compounds as ...
JWH-424
... which acts as a cannabinoid agonist at both the CB1 and CB2 receptors, but with moderate selectivity for CB2, having a Ki of ... JWH cannabinoids, Bromoarenes, Designer drugs, CB1 receptor agonists, All stub articles, Cannabinoid stubs). ... The heavier 8-iodo analogue is even more CB2 selective, with its 2-methyl derivative having 40 times selectivity for CB2. ... In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-424 are Schedule I Controlled ...
GPR55
This profile as a distinct non-CB1/CB2 receptor which responds to a variety of both endogenous and exogenous cannabinoid ... "Entrez Gene: GPR55 G protein-coupled receptor 55". Brown AJ (Nov 2007). "Novel cannabinoid receptors". British Journal of ... "The orphan receptor GPR55 is a novel cannabinoid receptor". British Journal of Pharmacology. 152 (7): 1092-101. doi:10.1038/sj. ... Later it was identified by an in silico screen as a putative cannabinoid receptor because of a similar amino acid sequence in ...
O-1918
... that appear to be related to the cannabinoid receptors. O-1918 is used in the study of these receptors, which have been found ... non-CB2 mediated effects that have become evident in the course of cannabinoid research. Abnormal cannabidiol Cannabidiol ... June 2010). "A cannabinoid receptor, sensitive to O-1918, is involved in the delayed hypotension induced by anandamide in ... March 2003). "Selective ligands and cellular effectors of a G protein-coupled endothelial cannabinoid receptor". Molecular ...
Endocannabinoid transporter
... whereas AMT activity instead is reduced by activation of the CB2 cannabinoid receptor, which inhibits NOS and NO release, also ... "Regulation by cannabinoid receptors of anandamide transport across the blood-brain barrier and through other endothelial cells ... and as cholesterol-dependent modulation of CB1 cannabinoid receptors in nerve cells. The catalytic efficiency (i.e., the ratio ... dependent modulation of type 1 cannabinoid receptors in nerve cells". Journal of Neuroscience Research. 81 (2): 275-283. doi: ...
CUMYL-FUBINACA
... with an EC50 of 1.8nM for human CB1 receptors and 23.7nM for human CB2 receptors, giving it around 13x selectivity for CB1. It ... January 2019). "Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex". Cell. 176 (3): 448-458.e12. doi:10.1016/j. ... Banister SD, Connor M (2018). "The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonist New Psychoactive ... CUMYL-FUBINACA (SGT-149) is an indazole-3-carboxamide based synthetic cannabinoid receptor agonist, ...
RQ-00202730
... is a benzimidazole derived drug that acts as a potent and highly selective agonist for the CB2 cannabinoid receptor ... Bow EW, Rimoldi JM (2016). "The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation". Perspectives ... with a Ki value of 19nM at CB2 and more than 4000x selectivity over CB1, though it also shows some activity as an antagonist of ... "Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome". ...
AM-1248
... is a drug that acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2, but with some ... cannabinoid receptor activity". Journal of Medicinal Chemistry. 53 (1): 295-315. doi:10.1021/jm901214q. PMID 19921781. US ... AM cannabinoids, Aminoalkylindoles, Piperidines, Adamantanoylindoles, Designer drugs, All stub articles, Cannabinoid stubs). ... The related compound 1-pentyl-3-(1-adamantoyl)indole was identified as having been sold as a cannabinoid designer drug in ...
Amyrin
... and anti-inflammatory properties in 2 models of persistent nociception via activation of the cannabinoid receptors CB1 and CB2 ... "Activation of cannabinoid receptors by the pentacyclic triterpene α,β-amyrin inhibits inflammatory and neuropathic persistent ...
JWH-250
JWH cannabinoids, Phenylacetylindoles, Phenol ethers, Designer drugs, CB1 receptor agonists, CB2 receptor agonists). ... The Cannabinoid Receptors. Edited by Patricia H Reggio. Humana Press 2009. ISBN 978-1-58829-712-9 "Understanding the 'Spice' ... an analgesic chemical from the phenylacetylindole family that acts as a cannabinoid agonist at both the CB1 and CB2 receptors, ... AM-2201 JWH-073 JWH-200 List of JWH cannabinoids List of AM cannabinoids MEPIRAPIM SDB-001 THJ-2201 Anvisa (2023-07-24). "RDC ...
JWH-249
JWH cannabinoids, Phenylacetylindoles, Bromoarenes, CB1 receptor agonists, CB2 receptor agonists, All stub articles, ... which acts as a cannabinoid agonist with about 2.4 times selectivity for CB1 with a Ki of 8.4 ± 1.8 nM and 20 ± 2 nM at CB2. ... In the United States, CB1 receptor agonists of the 3-phenylacetylindole class such as cannabipiperidiethanone are Schedule I ... Manera C, Tuccinardi T, Martinelli A (April 2008). "Indoles and related compounds as cannabinoid ligands". Mini Reviews in ...
5F-ADBICA
... is an indole-based synthetic cannabinoid that is a potent agonist at CB1 receptors and CB2 receptors with EC50 values of 0.77 ... Cannabinoids, Designer drugs, Indolecarboxamides, Organofluorides, All stub articles, Cannabinoid stubs). ... September 2015). "Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA ...
Yangonin
It has been shown to possess binding affinity for the cannabinoid receptor CB1 (Ki = 0.72 μM), and selectivity vs. the CB2 ... CB1 receptor agonists, GABAA receptor positive allosteric modulators, Monoamine oxidase inhibitors). ... The CB1 receptor affinity of yangonin suggests that the endocannabinoid system might contribute to the complex human ... Like other kavalactones, yangonin has been found to potentiate GABAA receptors. This may contribute to the anxiolytic ...
ICAM-1
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 ...
Cannabipiperidiethanone
CB1 receptor agonists, CB2 receptor agonists, All stub articles, Cannabinoid stubs). ... Its binding affinity was measured at the CB1 and CB2 receptors and it was found to have an IC50 of 591 nM at CB1 and 968 nM at ... as a designer drug in a herbal product and its affinity for cannabinoid CB₁ and CB₂ receptors". Chemical & Pharmaceutical ... In the United States, CB1 receptor agonists of the 3-phenylacetylindole class such as cannabipiperidiethanone are Schedule I ...
147
... which acts as a cannabinoid agonist at both the CB1 and CB2 receptors The maximum break, the highest possible break in snooker ...
JWH-251
JWH cannabinoids, Phenylacetylindoles, Designer drugs, CB1 receptor agonists, CB2 receptor agonists, All stub articles, ... which acts as a cannabinoid agonist with about five times selectivity for CB1 with a Ki of 29 nM and 146 nM at CB2. Similar to ... In the United States, all CB1 receptor agonists of the 3-phenylacetylindole class such as JWH-251 are Schedule I Controlled ... Manera C, Tuccinardi T, Martinelli A (April 2008). "Indoles and related compounds as cannabinoid ligands". Mini Reviews in ...
NMP-7
... is a drug which acts as both a non-selective agonist of the CB1 and CB2 cannabinoid receptors, and also as a blocker of T ... "Functional characterization and analgesic effects of mixed cannabinoid receptor/T-type channel ligands". Molecular Pain. 7: ... NMP-7 has an agonist EC50 of 96.9nM at CB1 and 10.5nM at CB2, and an IC50 of 1.84μM for blocking Cav3.2 T-type calcium channels ... Cannabinoids, Carbazoles, All stub articles, Cannabinoid stubs). ...
MDA-19
... in human cannabinoid receptors but functions differently in rat cannabinoid receptors binding to rat cannabinoid CB2 receptors ... MDA-19 is an agonist at human CB1 and CB2 receptors as well as rat CB1 receptors but functions as an inverse agonist in rat CB2 ... MDA-19 (also known as BZO-HEXOXIZID) is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB2, ... MDA-19 binds to human CB2 receptors at Ki = 43.3 +/- 10.3 nM and human CB1 receptors at Ki = 162.4 +/- 7.6 nM and functions as ...
SER-601
... (COR-167) is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, based on a quinolone-3- ... 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic ... with 190 times selectivity for CB2 over the related CB1 receptor. It has analgesic effects in animal studies, as well as ... and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ...