NPEC-caged-LY379268 is a type II mGluR agonist.

Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.

AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects.

TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate?dopamine D3?receptor (D3R)?antagonist with Ki values of 10.7?nM and?11.2 nM?at?rodent and human?D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with?pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.

PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.

Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and longlasting nonpeptide bradykinin B2 (BK2)?receptor antagonist. Fasitibant chloride hydrochloride has?proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis, et al.

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.

Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.

Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.

YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.

LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.

SKF-83566 is a potent,?blood-brain permeable and orally active D1-like dopamine receptor (D1DR)?antagonist and a weaker competitive antagonist at the vascular 5-HT2?receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50?of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.

SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 μM), P2X3 (12.9 μM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.

Tesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells.

5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptors agonist.

DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.

Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.

Clenproperol-D7 is the deuterium labeled Clenproperol. Clenproperol is a β2-adrenergic agonist.

Clenproperol is a β2-adrenergic agonist.

Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.

Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.

Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.

GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.