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β3-adrenergic receptors agonist
BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity. -
dopamine D2 receptor agonist
Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism. -
TGR5(GPCR19) agonist
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). -
adrenergic alpha-2 receptor agonist
Medetomidine Hydrochloride is an adrenergic alpha-2 receptor agonist, which is used in veterinary medicine for its analgesic and sedative properties. -
5-HT1A/1B and 5-HT2C agonist
RU 24969 hemisuccinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT. -
Guanylate cyclase C agonist
Linaclotide is a peptide agonist of the guanylate cyclase 2C. -
dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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prostacyclin receptor agonist
NS-304 is a selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors). -
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 Receptor agonist
Capadenoson is a selective agonist of adenosine-A1 receptor. -
5-HT6 agonist
WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM. -
dopaminergic agonist
Pergolide mesylate is a dopaminergic agonist that also decrease plasma prolactin concentrations. -
CB2 receptor agonist
Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials. -
β2-adrenoceptor agonist
Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effect. -
β-adrenoceptor agonist
Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma. -
I(1) imidazoline receptor agonist
Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist. -
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). -
5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. -
β2-adrenoceptor agonist
Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD). -
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. -
α-adrenergic receptor agonist
Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension. -
dopamine agonist
Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist. -
α2A-adrenoceptor agonist
Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. -
Nonimidazole inverse agonist
Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). -
Nonimidazole inverse agonist
Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). -
D2 receptor agonist
rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. -
LPA2 agonist
GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM). -
glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. -
EP2 Agonist
C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM. -
Serotonin2A Receptor Inverse Agonist
Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease. -
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. -
β2-adrenergic receptor agonist
Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD). -
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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Adenosine A Receptor agonist
2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively). -
mGluR agonist
(S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors. -
GLP-1 receptor agonist
Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist. -
Histamine H1-receptor agonist
Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.