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5-HT Receptor agonist
Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT). -
Alpha adrenergic agonist
Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist. -
Adrenergic Receptor agonist
Detomidine is a sedative with analgesic properties. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters. -
Adrenoceptors agonist
Dobutamine is a direct-acting agent whose primary activity results from stimulation of the β1-adrenoceptors of the heart, increasing contractility and cardiac output. -
β adrenoceptor agonist
Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline. -
mGluR Agonist
LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results. -
NOP receptor agonist
MCOPPB is a compound which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07. -
5-HT4-receptor agonist
Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist. -
alpha-1 adrenergic agonist
Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride. -
Dopamine Receptor Agonist
Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS). -
MT1/MT2-Receptor Agonist
Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor. -
α2 adrenergic agonist
Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist. -
Adrenergic Receptor agonist
Salbutamol sulfate (Albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. -
Adrenergic Receptor agonist
Synephrine (Oxedrine) is an amine compound commonly used for weight loss. -
5-HT Receptor agonist
Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo. -
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. -
Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
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Opioid Receptors agonist
BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM). -
β1-selective adrenergic receptor agonist
Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. -
D2 receptor agonist
B-HT 920 is a dopamine agonist that has been proposed as an antiparkinsonian agent. It also has α1-adrenergic and α2-adrenergic agonist activity. -
5-HT1B/1D receptor agonist
Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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α2-adrenoceptor agonist
Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). -
nonimidazole inverse agonist
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). -
CB1 receptor inverse agonist
Rimonabant hydrochloride is a CB1 receptor inverse agonist. -
Dopamine agonist
Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. -
CB1 receptor inverse agonist
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro. -
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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α1-adrenergic receptor agonist
Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure. -
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. -
imidazoline receptor 1 agonist
Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). Moxonidine causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure. -
5-HT Receptor agonist
Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.- Pierre Meschin, .et al. , Cell Calcium, 2015, Dec;58(6):549-57 PMID: 26427584
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beta2-adrenergic receptor agonist
Salmeterol is a long-acting beta2-adrenergic receptor agonist -
5-HT Receptor agonist
Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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adrenergic agonist
Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. -
β2-adrenergic receptor
Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties. -
alpha2-adrenoceptor agonist
Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
CB receptor agonist
WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.- Greish K, .et al. , J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922