SKF 38393 hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM[1].
PSB-603 is a potent and selective adenosine A2B receptor antagonist exhibiting a Ki value of 0.553 nM at the human A2B receptor and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1].
Hydrocortisone phosphate is the pharmaceutical term for cortisol, which is a steroid hormone, in the glucocorticoid class of hormones, increases blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrate.
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.[2].
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1].
A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM; does not evoke calcium responses in HEK293 cells expressing other FFARs, including GPR40, GPR41, GPR119, and GPR120; increases in intracellular calcium concentrations in HEK293/Gα16/GPR84 cells with EC50 of 1.01 uM; activates several GPR84-mediated signaling pathways, including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of ERK1/2, receptor desensitization and internalization, and receptor-β-arrestin interaction; reduces forskolin-stimulated cAMP accumulation in HEK293 cells with EC50 of 0.134 uM.
Galanin-Like Peptide (rat) is a 60 amino acid neuropeptide. Galanin-Like Peptide (rat) plays an important role in the regulation of feeding, body weight and energy metabolism[1].
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV[1].
Sograzepide (Netazepide;YF476) is a gastrin/cholecystokinin 2 receptor (CCK2) antagonist.
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
Norepinephrine tartrate (Levarterenol tartrate), a naturally occurring chemical in the body that acts as both a stress hormone and neurotransmitter, is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD)[1].
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis[1].
Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2].
L-Glutamic acid monosodium salt (Monosodium glutamate) is an activator of mGlu1 receptor.
2-Oleoylglycerol is a dietary naturally occurring lipid. 2-Oleoylglycerol is a GPR119 agonist, with an EC50 of 2.5 μM for human GPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol stimulates glucagon-like peptide-1 (GLP-1) secretion in vivo[1][2].
NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.Target: 5HT4 Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastro-oesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).In addition to its prokinetic properties, mosapride also exerts anti-inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects. Mosapride also promotes neurogenesis in the gastrointestinal tract which may prove useful in certain bowel disorders. The neurogenesis is due to mosapride's effect on the 5-HT4 receptor where it acts as an agonist.Its common side effects include dry mouth, abdominal pain, dizziness, headache, insomnia, malaise, nausea, diarrhoea and sometimes constipation. Unlike some other prokinetic agents, mosapride has little effect on potassium channels, no effect on hERG transfected cells, and no effect on cardiovascular function that could be detected in tests on humans. Due to the pharmacokinetics of mosapride, it would take 1,000 - 3,000 times the therapeutic dose to elicit cardiovascular effects.
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity[1][2][3].
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases[1].
ST91 is a α2-adrenoceptor (α2AR) agonist. ST91 activates both α2AAR and non-α2AAR subtypes to produce spinal antinociception[1][2][3].
Alfuzosin-d3 is deuterium labeled Alfuzosin.
Lubabegron is a potent modulator of β-adrenergic receptor (β -AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste[1].
GSK-269984B is a potent EP1 antagonist. GSK-269984B has the potential for inflammatory pain research[1].
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[1][2].
ISIS-2503, a 20-mer antisense oligonucleotide that inhibits Ha-Ras expression
Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system[1].
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist[1]. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8)[2].
CB1R Allosteric modulator 5, a novel1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity[1].
Timolol (hemihydrate) is a β-blocker available for both topical and systemic administration. Timolol (hemihydrate) is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension and Timolol (hemihydrate) also has cardioprotective effect[1][2].