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5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. -
CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
Sigma-2 receptor agonist
Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. -
A2A adenosine agonist
Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? -
opioid κ-selective agonist
Nalfurafine hydrochloride is a kappa-opioid receptor agonist- Lin Tian, .et al. , Research Square, 2023, May 30
- Alexander R French, .et al. , Pharmacol Biochem Behav, 2022, May;216:173377 PMID: 35364122
- Wen-Wen Zhang, .et al. , JCI Insight, 2022, Feb 8;7(3):e153191 PMID: 34914639
- A Dunn, .et al. , Psychopharmacology (Berl), 2020, May 20 PMID: 32435819
- Dunn AD, .et al. , ACS Chem Neurosci, 2019, Aug 21;10(8):3590-3600 PMID: 31313902
- Anika Mann, .et al. , Sci Signal, 2019, Mar 26;12(574). pii: eaau8072 PMID: 30914485
- Snyder LM, .et al. , Neuron, 2018, Sep 19;99(6):1274-1288.e6 PMID: 30236284
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Opioid Receptor Agonist
Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist -
β3-adrenergic receptor agonist
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). -
beta2-adrenergic agonist
Arformoterol tartrate is a beta2-adrenergic agonist -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
α2 adrenergic agonist
AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively. -
Sigma-2 receptor agonist
Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. -
Adrenergic Receptor agonist
Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels. -
D2 agonist
Naxagolide is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. -
dopamine D2-receptor agonist
ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug. -
ultra-long-acting β??? adrenoreceptor agonist
Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05. -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. -
A1 adenosine receptor agonist
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. -
α2- adrenoceptor antagonist / I2 imidazoline receptor agonist
Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively). -
imidazoline receptor 1 agonist
Moxonidine hydrochloride is a centrally acting antihypertensive agent. -
Adrenergic Receptor agonist
Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline. -
Adrenoceptors agonist
UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist. -
Adrenergic Receptor agonist
Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR. -
GPR40/FFA1 agonist
AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist. -
Kainate receptor agonist
Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms. -
5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors). -
D2 dopamine partial agonist
Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). -
SMO agonist
SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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2A-AR adrenergic agonist
Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand. -
EDG-1 (S1P1) agonist
CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM). -
histamine H3 receptor agonist
Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively). -
β3 adrenergic agonist
CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice.