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.

MRS 2219 is a selective potentiator of ATP-evoked responses at rat P2X1 receptors (EC50 = 5.9 μM).

MRS1191 is a selective A3 adenosine receptor antagonist.

ML218 HCl is a selective inhibitor of T-type calcium channels (IC50 values are 270 and 310 nM for Cav3.3 and Cav3.2 respectively in a patch EP assay). ML218 HCl decreases burst activity in STN neurons; reduces cataleptic behaviour in an in vivo rat model of Parkinson's disease.

ML169 is a novel, selective and brain penetrant M1 positive allosteric modulator (PAM).

LY456236 HCl is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). LY456236 HCl reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.

LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). LY 334370 hydrochloride displays antimigraine effects.

LY2087101 is an allosteric potentiator of α7, α4β2 and α4β4 nAChRs. LY2087101 displays selectivity against α3β4 nAChRs.

LY-165163 is a selective 5-HT1A and 5-HT1D serotonin receptor antagonists.

LP-44 is a high affinity 5-HT7 receptor agonist (Ki = 0.22 nM) that displays selectivity over 5-HT1A and 5-HT2A receptors (200- and > 1000-fold respectively). LP-44 dnduces relaxation of substance P-stimulated guinea pig ileum (EC50 = 2.56 μM).