Cannabinoidi

GAT229 is a CB1 positive modulator, enhancing CB agonist activity without direct activation; influences binding, signaling, and lowers ocular pressure in mice.

CB1-IN-2 (4g) inhibits CB1 receptor with 0.644 μM IC50; crosses blood-brain barrier, may cause CNS side effects like Rimonabant.

LEI-101: potent CB2 agonist, pEC50=8, bioavailable, >100x selective over CB1, potential for inflammatory diseases.

SMM-189 is a potent and selective CB2 inverse agonist.

Anandamide (AEA) is an endocannabinoid with neural reuptake. CAY10412, an AEA analog, inhibits this reuptake without binding to CB receptors.

VSN-16, a cannabinoid receptor agonist, is used potentially for the treatment of spasticity in multiple sclerosis.

UCM710 is a dual inhibitor of α/β hydrolase domain 6 (ABHD6) and fatty acid amide hydrolase (FAAH).

Modulates CB1R positively; inhibits cAMP production; strong β-arrestin-2 recruitment.

S-777469: Selective CB2 agonist, oral, inhibits itching in mice (Ki: 36 nM). Anti-pruritic.

CB1R modulator 1 (compound 11), a potent CB1R inhibitor, decreases activity of orthosteric ligands.

<p>CB1/2 agonist 4 is a potent CB1 full agonist (EC50: 15.09 nM) and CB2 partial agonist (EC50: 1.16 nM), with anti-pain and TRPV1 activation properties.</p>

Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid that acts as a ligand for VR1 and CB1, offering neuroprotective effects.

(R)-SLV 319: potent CB1 antagonist, K i of 894 nM, dextrorotatory isomer.

LH-21, a strong CB1 receptor antagonist, curbs eating and lessens weight gain in obese rats.

NIDA 41020 is a CB1 receptor antagonist.

AM6538: long-acting, high-affinity CB antagonist similar to rimonabant, useful for studying cannabinoid agonists.

In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand

AM6545 is a CB1 receptor antagonist used in the study of obesity and diabetes.

GP 2A is a selective agonist of CB2 receptor.

anandamide uptake inhibitor

CID1172084, a novel high-potent GPR55 agonist, interacts with cannabinoid receptors.

<p>COR167 is a CB2 agonist with immunomodulatory effects, protective brain properties, and antinociception.</p>

PGN36 (Compound 18) is a potent CB2 receptor antagonist with a high affinity (Ki=0.09 μM).

<p>CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.</p>

KLS-13019 is a highly effective and orally active GPR55 receptor antagonist, neuroprotective can reverse chemotherapy-induced peripheral neuropathy (CIPN).

GAT228, an allosteric ligand for the cannabinoid receptor 1 (CB1), functions as the enantiomer of GAT211 [1].

Ibipinabant (SLV319), a potent CB1 antagonist, K i = 7.8 nM, >1000x selective over CB2, for obesity and diabetic research.

CB1/2 agonist 2 binds tightly to cannabinoid receptors, acting fully on CB1 and inversely on CB2.

CB1 inverse agonist 2, an oral drug, counters CB1 effects, reducing CP55940-induced hypothermia and anorexia in mice.

<p>inverse agonist of CB2 receptors</p>

<p>Compound 18 is a potent CB1R allosteric modulator that acts as a negative modulator (NAM) for CB1R orthosteric ligands.</p>

ANEB-001 is an orally active CB1 inhibitor that can be used in studies of acute cannabinoid intoxication.

AZD1940 (UNII-0J0035E9FT) is a high affinity CB(1)/CB(2) receptor agonist of the cannabinoid with oral activity. Application in the study of orofacial pain.

PSB-CB5 (GPR18-IN-32)2 is a GRP18 antagonist with anti-inflammatory activity and can be used to study obesity and metabolic disorders.

CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.

<p>Inverse agonist of cannabinoid receptor CB1R. Taranabant was studied for its effect on smoking cessation and inducing weight loss. Serious adverse effects associated with this compound prevented further development as a drug in the clinic.</p>

<p>SCH-336: potent, selective CB2 agonist (Ki=1.8 nM, EC50=2 nM), orally active, 100x CB2 vs. CB1 preference, reduces leukocyte migration and eosinophilia.</p>

CB1 agonist 1 is a potent CB1 agonist with a pIC50 value of 5.7 for CB1 receptors.CB1 agonist 1 can be used to study brain disorders, pain, and inflammation.

JTE-907 是一种具有高度选择性和口服活性的 CB2 受体反向激动剂。JTE-907在体内展现出抗炎活性。

Nonabine is a compound with strong antiemetic properties that can be used to prevent nausea and vomiting associated with cancer chemotherapy.

<p>Olorinab (APD 371) (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.</p>

SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).

AM-1235 is a potent and selective cannabinoid receptor CB1 agonist.

CB2R PAM, an oral drug, boosts CB2 receptor response to specific agonists, showing potential in neuropathic pain relief.

11(Z),14(Z)-Eicosadienoic acid ethanolamide is an ethanolamide derivative of 11(Z),14(Z)-eicosadienoic acid.

Prostaglandin E2-1-glyceryl ester, a member of the Prostaglandin Glycerol Ester family, serves as an endocannabinoid ligand targeting the CB1 receptor. This compound triggers a swift and transient surge in intracellular free calcium levels [1] [2].

O-Arachidonoyl glycidol (compound 1), a 2-arachidonoylglycerol (2-AG) analog, effectively inhibits the hydrolysis of cytosolic 2-oleoylglycerol (2-OG) with an IC50 value of 4.5 µM, and also blocks 2-OG and anandamide hydrolysis in membrane fractions with IC50 values of 19 µM and 12 µM, respectively [1].

COR659: suppresses alcohol/chocolate intake in rats; enhances GABAB receptor, blocks CB1 receptor.

GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.

PSB-SB1202 (Compound 21a), a phenyl coumarin compound, acts as a CB1/CB2 agonist. It demonstrates EC50 values of 56 and 14 nM and K i values of 32 and 49 nM for CB1 and CB2 receptors, respectively [1].

SAD-448 is a cannabinoid receptor type 1 (CB1) agonist. SAD-448 controls spasticity via action on the peripheral nerve CB1 receptor.

CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.

O-2050: strong CB1 antagonist (Ki 2.5 nM), CB2 inhibitor (Ki 0.2 nM); reduces mouse food intake, increases activity.

MRL-650 is an oral, selective CB1 agonist; IC50: CB1=7.5 nM, CB2=4100 nM; anorexigenic effects noted.

<p>(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].</p>

CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and

CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively.

PF 514273 is a CB1 receptor antagonist.

GSK494581A is a GPR55 agonist and glycine transporter subtype 1 inhibitor.

O-2545 is a potent water-soluble central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptor agonist with Ki values of 1.5 and 0.32 nM, respectively. Typically, cannabinoid agonists are highly lipophilic and require solubilization through surfactant agents or binding to water miscible substances like albumin, Tween 80, or Emulphor for use. When dissolved in saline, O-2545 has shown high efficacy in mouse behavioral models, administered either intravenously or intracerebroventricularly.

GW405833 hydrochloride, a potent and selective agonist of the cannabinoid-2 (CB2) receptor (EC 50 = 0.65 nM; maximum inhibition = 44.6%), exhibits significant antihyperalgesic effects in various rodent pain models [1] [2] [3].

2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an "entourage" effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.

Heptadecanoyl ethanolamide, an endogenous cannabinoid, serves as a synthetic analog of PEA, featuring an odd-numbered (17-carbon) fatty acid chain [1].

Tedalinab is an effective and selective cannabinoid receptor 2 agonist.

Tricosanoyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, has an ethanolamine metabolite whose significance remains to be established.

Hemopressin(rat) TFA, a nonapeptide from hemoglobin α1-chain, selectively inhibits CB1 receptors and reduces inflammatory pain.

CB-25 is a partial agonist ligand of CB1 cannabinoid receptors, augmenting Forskolin-induced cAMP formation in cancer cells, though not affecting hCB1-CHO cells

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

γ-Linolenoyl monoethanolamide, a fatty N-acyl ethanolamine, acts as an endocannabinoid [1] [2].

PF-03550096, an orally active synthetic cannabinoid (CB), selectively binds to peripheral CB2 receptors with a Ki value of 7.9 nM, demonstrating analgesic activity [1].

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.

AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor.

URB447, a peripherally restricted CB1 cannabinoid antagonist with IC50 values of 313 nM for rat CB1 receptor and 41 nM for human CB2 receptor, effectively reduces food intake and body weight gain in mice. It achieves these effects without penetrating the brain or antagonizing central CB1-dependent responses, making it a potential research tool for obesity studies [1].

<p>CB-52 acts as a neutral antagonist and ligand for the CB2 cannabinoid receptor [1].</p>

Amauromine is a peripherally selective and potent cannabinoid receptor type 1 (CB1) receptor antagonist, a novel alkaloid with vasodilatory activity.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester functioning as a central cannabinoid receptor (CB1) antagonist and exhibits

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).

<p>GP 1a: potent CB2 receptor agonist (EC50=7.1), 30x CB2 over CB1 preference, boosts P-ERK1/2, aids skin healing, anti-inflammatory.</p>

<p>GW 833972A: selective CB2 agonist; reduces neural depolarization and citric acid cough in animals.</p>

<p>Cannabichromevarin is a phytocannabinoid naturally found in very low levels compared to other cannabinoids from which it differs in having a propyl chain in place of a pentyl chain1. Based on its structure, it is believed to act as a potent anandamine inhibitor similarly to cannabichromene, however, the majority of its pharmacological and toxicological properties are currently unknown. In vitro assays have shown cannabichromevarin protect against oxidative stress in vitro in macrophages2. It was recently shown to be effective for treatment-resistant epilepsy in a patented combination with cannabidiol in a recent open-ended clinical trial3.</p>

Ac-Atovaquone, an ester-acetylated derivative of atovaquone, acts as a potent inhibitor of cytochrome bc1 (cytochrome bc1). This compound shows potential for use in malaria research.

Compound 29 is a potent, CB2-selective antagonist/reverse agonist. Derivatives 23 & 24 offer antinociception; 24 activates cannabinoid/TRPV1 receptors.

<p>Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.</p>

MDMB-FUBICA is a potent agonist of the cannabinoid receptors and exhibits psychoactive properties. It can be utilized in e-cigarettes.

AM8936: potent CB1 agonist, EC50 rCB1=8.6nM/hCB1=1.4nM, Ki rat CB1=0.55nM; potential for CNS, metabolic, pain, glaucoma research.

BNS808 is an orally active, selective CB1R antagonist with an IC50 of 0.8 nM, demonstrating significant selectivity for CB2R and minimal brain penetration. It is being studied for the treatment of obesity and related metabolic complications, such as metabolic dysfunction-associated steatotic liver disease (MASLD). BNS808 reduces drug exposure to the central nervous system, enhancing safety, and minimizes drug interactions through high plasma protein binding.

Bzo-poxizid is a synthetic cannabinoid and a psychoactive substance.

CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.

Cannabigerovarin (CBGV) is a compound categorized as a phytocannabinoid.

PSB-KK1415 is a selective agonist for the human orphan G protein-coupled receptor GPR18, with an EC50 of 19.1 nM.

<p>HU 433, a synthetic cannabinoid, acts as a CB2 receptor agonist and is an enantiomer of HU 308. It provides anti-inflammatory and neuroprotective effects by binding to the CB2 receptor, primarily found on immune cells, thereby modulating immune responses and inflammation. Additionally, HU 433 influences microglial signaling pathways, particularly LPS and IFNγ-mediated routes, affecting the phosphorylation of MAPKs, including ERK1/2, JNK, p38, and Akt. This compound is valuable in researching neuroinflammation and retinal diseases.</p>

AM11638 is an endogenous cannabinoid analogue that targets cannabinoid receptors (CB1 and CB2 receptors), exhibiting analgesic properties. It shows potential for research in neurological disorders and inflammation-related diseases.

<p>CB1 antagonist 4 is an inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. It can reduce body weight, improve plasma inflammatory markers, and enhance glucose homeostasis [1].</p>

<p>HU-308, a synthetic cannabinoid analogue, is a highly selective agonist of the CB2 receptor. It demonstrates an affinity for the CB2 receptor that is over 440 times greater than its affinity for the CB1 receptor, which are predominantly found in immune cells. This compound plays a crucial role in modulating the immunosuppressive effects of the endocannabinoid system (ECS). Additionally, HU-308 possesses anti-inflammatory and neuroprotective properties, and it regulates the function of microglia. Its potential applications include research into neuroinflammation and retinal diseases.</p>

<p>MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2), demonstrating an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. The compound exhibits good affinity for CB2 receptors, with Ki values of 422 nM for humans and 238 nM for rats. In rat models, MDA7 shows analgesic activity.</p>

CBR Agonist-1 targets CB1R and CB2R with Ki of 0.18 μM and 1.22 μM, useful for studying cannabinoid-related diseases.

GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) & 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.

BAY 38-7271: potent neuroprotective, selective CB1/CB2 agonist, Ki of 1.85 nM (CB1) & 5.96 nM (CB2).

1'-Naphthoyl-2-methylindole (Compound 88) acts as a cannabinoid mimic and an inhibitor of Win 55212-2, displaying a 34% inhibition of [3H]Win 55212-2 binding to cannabinoid receptors at a concentration of 3 μM.

<p>FDU-PB-22, a novel synthetic cannabinoid, undergoes rapid metabolism in human liver microsomes (HLM) with a half-life of 12.4 minutes.</p>

MDA77 is a CB2 agonist with an EC50 value of 5.82 nM and exhibits no activity towards CB1.

AB-FUBINACA 3-fluorobenzyl isomer is a synthetic cannabinoid and an indazole derivative, exhibiting high affinity for central CB1 receptors (Ki= 0.9 nM) and possessing anticonvulsant activity.

CBR Agonist-2: CB1 receptor agonist, EC50 - 960 nM, Ki - 970 nM, useful for hCB1R-related disease research.