Catalog No.
Product Name
Application
Product Information
Citations
-
5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. -
A1 adenosine receptor agonist
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. - Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
-
guanylate cyclase activator
(4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued. - Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
-
AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
CaSR antagonist
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. -
5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
-
Opioid Receptors agonist
BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM). -
Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
5-HT3 antagonist
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. - Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
-
CGRP receptor antagonist
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. -
Opioid antagonist
Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract. -
D2 receptor antagonist
Adoprazine is part of the Antidepressant Agent group -
Endothelin antagonist
Avosentan (SPP301) is a potent and highly selective ETA receptor blocker. -
Serotonin 5HT3-receptor antagonist
Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. -
CaSR activator
AMG-073 (Cinacalcet) represents a new class of compounds for the treatment of hyperparathyroidism. -
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. -
mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. -
glucagon receptor antagonist
Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist. -
KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. -
DP1 inhibitor
Laropiprant is used in combination with niacin to reduce blood cholesterol. Laropiprant acts as a DP1 antagonist, reducing the vasodilation. -
mGluR-2 antagonist
LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a. -
CysLT1 receptor antagonist
Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist. -
Endothelin receptor antagonist
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
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).
