b1 receptor

Bradykinin B1 Receptor Antagonist 1 (compound 6B) is a potent bradykinin B1 antagonist that can cross the blood-brain barrier. It holds potential for pain research.

ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors.

SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).

[Des-Arg9]-Bradykinin ([Des-Arg9]-Bradykinin(2TFA))(2TFA) is an agonist of Bradykinin (B1) receptor.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence.

Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1/FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

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.

CB1R agonist 1 (Compound '1350) is a potent full agonist of the cannabinoid-1 receptor (CB1R) with a Ki value of 0.95 nM. It demonstrates significant pain-relieving effects in various pain models, including acute thermal pain, inflammatory pain, and neuropathic pain.

(±)5(6)-EET Ethanolamide is a metabolite derived from Anandamide through oxidation by cytochrome P450 enzymes. It acts as a selective cannabinoid receptor 2 (CB2) agonist. The Ki values for (±)5(6)-EET Ethanolamide against human CB1 and CB2 are 11.4 μM and 8.9 nM, respectively. This compound can be used in studies related to immunoregulation and neuroinflammation.

MJ 15 is a CB1 receptor antagonist with specificity for the study of obesity-induced diseases.

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.

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

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

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

CB1/2 agonist 1 is a potent CB1/2 agonist that crosses the blood-brain barrier, acting on CB1R (EC50: 56.15 nM) and CB2R (EC50: 11.63 nM). It reduces glutamate release and LPS-induced microglia activation, exhibiting anti-inflammatory and analgesic activities, with potential for multiple sclerosis studies.

N-Arachidonyldopamine (NADA) is a selective and potent endogenous CB1 receptor agonist (Ki: 250 nM).N-Arachidonyldopamine is also a potent and selective TRPV1 agonist with an EC50 value of ~50 nM.