Diphenylpyraline Hcl is a first-generation antihistamine with anticholinergic effects, acts as a dopamine reuptake inhibitor, shows to be useful in the treatment of Parkinsonism.
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].
TCS 2510 is a selective EP4 agonist. TCS 2510 can be used for the research of metabolic diseases[1].
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM, which is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM)[1].
LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.
Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1)[1].
CGS 15943 is an adenosine A2 receptor antagonist and reduces stroke injury in the Mongolian gerbil[1]. CGS 15943 is a selectively p110γ inhibitor with an IC50 of 1.1 μM, shows inhibitory effect on p110δ (IC50=8.47 μM), has an anti-carcinogenic effect on HCC and PDAC cells[2].
NPEC-caged-LY379268 is a type II mGluR agonist[1].
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[1][2].
CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity[1].
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.
Aprophen (Aprofene) is an antimuscarinic inhibitor. Aprophen can be used for the research of central nervous system[1].
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease[1][2].
S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4[1][2].
β-Lipotropin (61-69) is a potent opioid agonist[1][2].
RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment[1].
Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma[1][2][3][4][5][6].
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM[1].
Atipamezole hydrochloride is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.
Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.
Famotidine-13C,d3 is the 13C- and deuterium labeled. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM[1].
Deslorelin is a GnRH agonist. Deslorelin implants can be used as an alternative to dopamine agonists to induce fertil eoestrus in the bitch in anoestrus. The deslorelin implant can be used successfully in the queen for oestrus inhibition. Deslorelin acetate did not significantly affect the spontaneous contraction amplitude but caused a decrease in the frequency in the dorsal and ventral parts of the bladder.
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats[1].
Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II[1]. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca2+ levels. Angiotensin II also acts at the Na+/H+ exchanger in the proximal tubules of the kidney[2][3].