Protease-Activated Receptor-1, PAR-1 Agonist is a thrombin-specific, protease-activated receptor 1 (PAR-1)-specific agonist peptide[1].
Oxytocin (α-Hypophamine) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
Tezosentan-d4 (RO 610612-d4) is the deuterium labeled Tezosentan. Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively[1][2].
N6-[2-(4-Aminophenyl)ethyl]adenosine is a potent, non-selective A3 adenosine receptor agonist.Target: Adenosine receptor agonist.in vitro: N6-[2-(4-Aminophenyl)ethyl]adenosine is a non-selective agonist of the adenosine A3 receptors, at the subprotective dose of 1 mg/kg against electroconvulsions, significantly potentiates the anticonvulsive action of phenobarbital, diphenylhydantoin and valproate against maximal electroshock, being ineffective at lower doses. N6-[2-(4-Aminophenyl)ethyl]adenosine (0.0039-1 mg/kg) also enhances the protective activity of carbamazepine. N6-[2-(4-Aminophenyl)ethyl]adenosine at low doses potentiates the protective activity of Carbamazepine most likely through the A subtype of adenosine receptors. At higher doses, N6-[2-(4-Aminophenyl)ethyl]adenosine seems to enhance the anticonvulsive effect of other antiepileptics via adenosine A1 receptors. [1]in vivo: N6-[2-(4-Aminophenyl)ethyl]adenosine (2-4 mg/kg) has no significant effect on seizure parameters (seizure severity, seizure duration and afterdischarge duration) in amygdala-kindled rats. N6-[2-(4-Aminophenyl)ethyl]adenosine is combined with antiepileptic drugs administered at doses ineffective in fully kindled rats.[2]
Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.IC50 Value: 0.92 uM (Ki with glycolaldehyde as the varied substrate for E3)Target: H2 receptorMetiamide is an intermediate compound in the development of the successful anti-ulcer drug cimetidine. in vitro: Metiamide is a competitive with aldehyde substrates and noncompetitive with the Human E3 Aldehyde Dehydrogenase coenzyme, binding to both the free E3 isozyme and the enzyme·coenzyme binary complex withK i values of 0.92 μM glycolaldehyde as the varied substrate[1]. Data was got as percentage change in GTPase activity induced by metiamide compared with the GTPase activity stimulated by HA (100 μM)[2]. in vivo: Metiamide is a histamine H2-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. Metiamide inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Metiamide include an increase in gastric bacterial flora such as nitrate-reducing organisms.
GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.IC50 value: 3.1 nM(Ki)Target: adenosine A1 receptorin vitro: GR79236 is a highly potent and selective A1-receptor agonist that is originally developed for the treatment of Type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases.in vivo: GR79236 has also been shown to have antinociceptive and anti-inflammatory properties in animal models. GR79236 inhibits the release of CGRP evoked by superior sagittal sinus (SSS) stimulation in the cat and inhibits trigeminal nucleus firing in the cat and rat. GR79236X has acute, short-term analgesic efficacy.
Nitrosoglutathione (GSNO), a exogenous NO donor and a substrate for rat alcohol dehydrogenase class III isoenzyme, inhibits cerebrovascular angiotensin II-dependent and -independent AT1 receptor responses[1][2][3][4].
OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 2 inhibitis IP3-Synthesis, rat OT-R (IC50 = 0.33 μM).IC50 value: 0.33μMTarget: oxytocin receptor
TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened drug targets[1]. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells[2].
Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.IC50 value: 1.28 uM (inhibition of AVP-induced platelet aggregation)Target: vasopressin receptor 2Tolvaptan (OPC-41061) is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. Tolvaptan (OPC-41061) is used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.
(R)-Terazosin is the R-enantiomer of Terazosin. (R)-Terazosin is a potent α-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively[1].
A68930 hydrochloride, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis[1].
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity[1].
PF-610355 is a long-acting inhaled β2-adrenoreceptor agonist, with an EC50 of 0.26 nM. PF-610355 has the potential for the study of asthma and COPD[1].
Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues[1][2][3].
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.Target: A2A adenosine receptorRegadenoson produces hyperemia quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging. The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.Regadenoson has a 2 to 3 minute biological half-life.[1]
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
(-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3. (-)-Penbutolol can increase hippocampal 5-HT output[1][2].
GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM [1].
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production[1]. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM[1].
H3 receptor antagonist 1 is an antagonist of histamine H3 receptor, used in the research of neurological disease.
d[Cha4]-AVP is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
[Tyr(P)4] Angiotensin II is a peptide that has multiple effects on vascular smooth muscle, including contraction of normal arteries and hypertrophy or hyperplasia of cultured cells or diseased vessels[1].
Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM[1]. (+)-Penbutolol is an optical isomer of l-penbutolol with Na+ channel-blocking action[2].
MF266-3 is a potent, selective prostaglandin E receptor subtype 3 (EP3) antagonist with Ki of 0.8 nM; displayes a relatively good selectivity over other prostanoid receptors.
Azilsartan mopivabil is the potent antagonist of angiotensin II receptor[1].
Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor.
P4pal10 is a PAR4 antagonist. P4pal10 prevents the thrombin-mediated aggregation of mouse platelets in vivo. P4pal10 significantly reduced both the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474)[1].