SQ-29548 is a highly selective TP receptor antagonist which binds to the human recombinant TP receptor with a Ki of 4.1 nM. SQ-29548 inhibits the aggregation of washed human platelets induced by U-46619 with an IC50 of 0.06 μM.

SNAP5089 is a subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels).

SM 21 is a novel sigma(2) antagonist.

SM19712 is a nonpeptide endothelin converting enzyme inhibitor.

SKF-83959 HBr is a dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). SKF-83959 HBr may act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonizing the behavioral effects of cocaine.

SKF-81297 HBr is a selective dopamine D1 receptor agonist, which stimulates motor behaviour of MPTP-lesioned monkeys.

SKF-75670 hydrobromide is a atypical D1DR (dopamine receptor) agonist. It displays antagonist activity in vitro and agonist activity in vivo.

SIB-1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. It positive allosteric modulator at mGlu4 receptors.

SIB-1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype. SIB-1757 displays an IC50 value of 0.4 μM at hmGlu5 compared with > 30 μM at hmGlu1b, hmGlu2, hmGlu4, hmGlu6, hmGlu7 and hmGlu8.

RU 28318, potassium salt is a potent and selective antagonist for the mineralocorticoid receptor (MR). RU 28318, potassium salt inhibits aldosterone production and secretion, and selectively decreases ex-vivo MR binding in the hippocampus of adrenalectomised rats. It also decreases blood pressure in female rats following central administration in vivo.

Ro67-7476 is a positive allosteric modulator of mGlu1 receptors. It potentiates glutamate-induced calcium release (EC50 = 60.1 nM at rat mGluR1a). Ro67-7476 displays no activity at human mGlu1 receptors.

PF0998425 is a bioactive chemical.

PF-04859989 HCl is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid. PF-04859989 HCl has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder.

PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines). It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.

PD-156707 is an endothelin A receptor-selective antagonist.

m-Methylphenylacetonitrile is a bioactive chemical.

NS3763 is a noncompetitive antagonist of GLUK5 receptor. NS3763 displays selectivity for inhibition of domoate-induced increase in intracellular calcium mediated through the GLU(K5) subtype (IC(50) = 1.6 microM) of kainate receptors compared with the GLU(K6) subtype (IC(50) > 30 microM). NS3763 inhibits the GLU(K5)-mediated response in a noncompetitive manner. NS3763 selectively inhibits l-glutamate- and domoate-evoked currents through GLU(K5) receptors in HEK293 cells.

NS1738 is a α7 positive allosteric modulator.

NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket.

NNC269100 is a somatostatin sst4 receptor agonist that displays > 100-fold selectivity over sst2 receptors (Ki values are 6 and 621 nM for sst4 and sst2 receptors respectively). NNC269100 potently inhibits forskolin-induced cAMP accumulation (EC50 = 26 nM).

NNC052090 is a GABA uptake inhibitor that displays moderate selectivity for BGT-1 (mGAT-2) transporters (Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively). NNC052090 inhibits sound-induced tonic and clonic convulsions in DBA/2 mice. NNC052090 also displays affinity at α1- and D2-receptors (IC50 values are 266 and 1632 nM respectively).

NGD 94-1 is a high affinity D4 receptor ligand. NGD 94-1 is selective over D1, D2, D3 and D5 receptors. NGD 94-1 displays antagonist activity at the human D4.2 receptor (Ki = 3.6 nM in transfected CHO cells) and exhibits agonist activity at the D4.4 receptor in HEK 293 cells.

NGB2904 is a potent and selective dopamine D3 receptor antagonist (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes quinpirole-stimulated mitogenesis (IC50 = 6.8 nM)

NF449 is a potent purinergic receptor antagonist that displays high selectivity for P2X1 (IC50 values are 0.28, 0.69, 120, 1820, 47000 and > 300000 nM for rP2X1, rP2X1+5, rP2X2+3, rP2X3, rP2X2 and P2X4 receptors respectively). NF449 provides antithrombotic protection in vivo. NF449 also acts as a Gsα-selective antagonist.

NE58043 is a bioactive chemical.

NE58018 is a bioactive chemical.

MRS5698 is a high affinity and selective A3 adenosine receptor agonist (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors. MRS5698 reverses mechanoallodynia in several neuropathic pain models in vivo.

MRS 4062 triethylammonium salt is a selective P2Y4 receptor agonist (EC50 values are 23, 640, and 740 nM for hP2Y4, hP2Y2 and hP2Y6 respectively).

MRS2905 is a bioactive chemical.

MRS 2693 trisodium salt is a selective P2Y6 agonist (EC50 = 0.015 μM at the hP2Y6 receptor). MRS 2693 trisodium salt displays no activity at other P2Y subtypes.