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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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Opioid Receptor agonist
ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM. -
β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. -
Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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CaSR agonist
Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid. -
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. -
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 -
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. -
5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors). -
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. -
β3-adrenergic receptors agonist
BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity. -
NMDA& mGlu receptor agonist
Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist. -
GLP-1 receptor agonist
ixisenatide inhibit glucagon release, markedly reduce postprandial glucago. have a promoting effct in diabetes mellitus (T2DM). -
Adenosine A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
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Dopamine receptor agonist
(+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM). -
μ-opioid receptor agonist
Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
μ-opioid receptor agonist
Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
LPA2 agonist
GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM). -
EP2 Agonist
C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM. -
5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
dopamine D2 receptor agonist
UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.- Anika Mann, .et al. , Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
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GLP-1 receptor agonist
Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist. -
REV-ERBα/β agonist
SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM. -
β-adrenoceptor agonist
Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist. -
GLP-1 agonist
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).- Tito Borner, .et al. , Cell Rep, 2020, Jun 16;31(11):107768 PMID: 32553160
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Endogenous galanin receptor agonist
Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects -
5-HT(2A) receptor agonist
Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis. -
beta-adrenergic agonist
Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent. -
Somatostatin Receptor agonist
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). -
angiotensin 1 (AT1) and AT2 receptor agonist
Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist. -
β3-adrenoceptor agonist
Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity. -
Adenosine receptor agonist
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.