R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea[1].
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect[1][2][3][4].
DV-7028 is a selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist[1].
ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 ± 4.3 nM.Target: mAChRScopolamine (USAN), also known as levo-duboisine and hyoscine, sold as Scopoderm, is a tropane alkaloid drug with muscarinic antagonist effects. It is among the secondary metabolites of plants from Solanaceae (nightshade) family of plants, such as henbane, jimson weed (Datura), angel's trumpets (Brugmansia), and corkwood (Duboisia). Scopolamine exerts its effects by acting as a competitive antagonist at muscarinic acetylcholine receptors, specifically M1 receptors; it is thus classified as an anticholinergic, antimuscarinic drug. Its use in medicine is relatively limited, with its chief uses being in the treatment of motion sickness and postoperative nausea and vomiting. Scopolamine is named after the plant genus Scopolia. The name "hyoscine" is from the scientific name for henbane, Hyoscyamus niger.
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation[1][2].
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist[1]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo[2].
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
Tripelennamine Hcl, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.IC50 Value:Target: Histamine H1 receptorTripelennamine can be used in the treatment of asthma, hay fever, rhinitus and urticaria.in vitro: Arterial and mixed venous blood-gas and pH measurements were made at rest before and after saline or drug administration and during incremental exercise leading to maximal exertion at 14 m/s on 3.5% uphill grade for 120 s. Galloping at this workload elicited maximal heart rate and induced exercise-induced pulmonary hemorrhage in all horses in both treatments, thereby indicating that capillary stress failure-related pulmonary injury had occurred [1].in vivo: The data obtained (median and range in brackets) in camels and horses, respectively, were as follows: the terminal elimination half-lives were 2.39 (1.91-6.54) and 2.08 (1.31-5.65) h, total body clearances were 0.97 (0.82-1.42) and 0.84 (0.64-1.17)L/h/kg. The volumes of distribution at steady state were 2.87 (1.59-6.67) and 1.69 (1.18-3.50) L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model were 1.75 (0.68-2.27) and 1.06 (0.91-2.20) L/kg [2]. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively [3].
KFM19 is a potent, selective Adenosine receptor (A1-receptor) antagonist, with an IC50 of 50 nM.
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation[1][2][3].
Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation[1].
CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM[1].
Bometolol Hydrochloride is a beta-adrenergic blocking agent, used for the research of cardiovascular disease.
Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
A novel potent gonadotrophin releasing hormone (GnRH) antagonist.
GW 833972A is a selective CB2 receptor agonist. GW 833972A inhibits induced nerve depolarization and citric acid-induced cough in animal models[1].
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively[1].
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[1].
Eprosartan is a nonpeptide angiotensin II receptor antagonist with IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively. IC50 Value: 9.2 nM(in rat adrenal cortical membranes); 3.9 nM(in human adrenal cortical membranes)Target: Angiotensin Receptor Type-1(AT1)in vitro: Eprosartan mesylate, is one of the highly selective, orally active, non-peptide angiotensin-II-receptor antagonists [1]. In rat and human adrenal cortical membranes, Eprosartan displaced specifically bound [125I]AII with IC50 of 9.2 and 3.9 nM, respectively. Eprosartan also inhibited [125I]AII binding to human liver membranes (IC50 = 1.7 nM) and to rat mesenteric artery membranes (IC50 = 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca++ levels. In rabbit aortic rings [2].in vivo: Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr. In this same rat model, Eprosartan had no effect on base-line pressure or on the pressor response to norepinephrine or vasopressin [2]. Eprosartan is highly effective and safe in lowering blood pressure, notably SBP, in older subjects with mild to moderate hypertension [3]. Treatment with eprosartan in once-daily doses up to 1200 mg alone or in combination with HCTZ was well tolerated, with dizziness and asthenia being the most common side effects [4]. Therapy with eprosartan mesilat was associated with significant hypotensive effect (more evident in patients with high systolic blood pressure), improvement in 24-hour blood pressure profile and quality of life, and lower probability of secondary stroke. Side effects were not observed [5].
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor[1]. BMS-984923 is a potent mGluR5 silent allosteric modulator[2].
Clonidine-d4 is the deuterium labeled Clonidine. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent[1][2][3][4][5].
MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.target: 2-SORA [1]In vivo: MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. The reference for animal administration is 30 mg/kg. [2]
NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM[1].
NAN-190 is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.Target: 5-HT in vitro: NAN-190 is a 5-HT1A antagonist. [3] NAN-190 is a selective antagonist of 5-HT1A. [1]in vivo: NAN-190 (0.5 mg/kg, ip), as a 5-HT1A receptor antagonist, is injected concomitantly with the effective dose of fluoxetine. NAN-190 (5-HT1A receptor antagonist) reverses the catalepsy-improving effect of fluoxetine in 6-OHDA lesioned rats. [2]
Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, reduces several effects of tetrahydrocannabinol (THC).
AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1].
SB 277011A dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
[D-Phe12,Leu14]-Bombesin is an antagonist of Bombesin Receptor. [D-Phe12,Leu14]-Bombesin can be used for the research of cancer[1].
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation[1][2].