Catalog No.
Product Name
Application
Product Information
Citations
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5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
prostaglandin EP4 receptor antagonist
Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. -
Opioid antagonist
Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
CysLT1 receptor antagonist
MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. -
CCK-2 receptor antagonist
Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
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). - cAMPS-Sp, triethylammonium salt is a cell-permeable cAMP analog that activates cAMP receptor proteins such as PKA and cAMP-regulated guanine nucleotide exchange factor.
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dopaminergic stabilizer
ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission. -
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 blocking agent
Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. -
Histamine H1-receptor agonist
Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. - Docusate Sodium is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.
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serotonin/histamine2 antagonist
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2. -
dopamine (D2) receptor antagonist
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents. -
α1D Adrenoceptor Antagonist
TAK-259 is a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist (α1D, Ki = 1.1 nM) with Anti-urinary Frequency Effects and Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. -
V1b receptor antagonist
Vasopressin antagonist, Orally available and selective V1b receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over hV1a, hV2, and hOT). -
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. -
CB1/CB2 receptor agonist
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . -
5-HT1A receptor agonist/serotonin reuptake inhibitor
YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively. -
β-adrenergic receptors antagonist
Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. -
H1 histamine receptor antagonist
Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor. -
Dopamine receptor antagonist
Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting. - Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
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Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. -
5-HT3 receptor antagonist
Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. -
Histamine/cholinergic inhibitor
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. -
angiotensin II receptor type 1 antagonist
Azilsartan medoxomil is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. -
Adenosine A2 receptor agonist
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. -
β2-adrenergic receptor agonist
Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect. -
Histamine H1 receptor antagonist
Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity. -
5-HT1A receptor antagonist/COMT inhibitor
Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. -
β-adrenoceptor agonist
Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
