Catalog No.
Product Name
Application
Product Information
Citations
-
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.
-
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 . - Prostaglandin F2α is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
- Michel R Corboz, .et al. , Prostaglandins Other Lipid Mediat, 2020, Oct 1;152:106486 PMID: 33011365
-
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.
-
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. -
Serotonin reuptake inhibitor
Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. -
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. -
nonpeptide vasopressin V2 receptor antagonist
Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM. -
LPA1 antagonist
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. -
orexin OX1 receptor antagonist
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. - Serotonin is a monoamine neurotransmitter that is biochemically derived from tryptophan and produced in serotonergic neurons in the central nervous system and in enterochromaffin cells in the gastrointestinal tract.
-
H1-receptor antagonist
Tripelennamine hydrochloride, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine. -
5-HT (serotonin)/dopamine receptor antagonist
Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
GPR55 antagonist
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. -
A2 receptor antagonist
Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor. -
A2AR antagonist
AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. -
A1 adenosine receptors antagonist
Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 μM for platelets). -
Adenosine receptor antagonist
Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. -
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
