Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
Fenoterol hydrobromide is a β 2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.
Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
Ensaculin free base (KA-672) is a NMDA antagonist and have high affinities to serotonergic 5-HT1A and 5-HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems[1].
Esmolol Hydrochloride is a beta adrenergic receptor blocker.Target: Adrenergic receptorEsmolol Hydrochloride is the hydrochloride salt form of Esmolol, a short and rapid-acting beta adrenergic antagonist belonging to the class II anti-arrhythmic drugs and devoid of intrinsic sympathomimetic activity. Esmolol hydrochloride competitively blocks beta-1 adrenergic receptors in cardiac muscle and reduces the contractility and cardiac rate of heart muscle, thereby decreasing cardiac output and myocardial oxygen demands. This agent also decreases sympathetic output centrally and blocks renin secretion. At higher doses, Esmolol hydrochloride also blocks beta-2 receptors located in bronchial and vascular smooth muscle, thereby leading to smooth muscle relaxation.
Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].
SB-226552 is an aryloxypropanolamine selective beta3AR agonist.
Ko-3290 is an antagonist of β-adrenoceptor, with cardioselectivity and antilipolytic effects in animals.
Aposcopolamine is an alkaloid that can be isolated from Datura ferox. Aposcopolamin can closely binds with ACHE, ADRA2A and CHRM2. Aposcopolamine can be used for the research of Alzheimer's disease[1].
(Rac)-Dobutamine-d6 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner[1][1].
Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α，5-HT1β and 5-HT2，respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].
Clozapine-d4 (HF 1854-d4) is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
Xylometazoline Hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.Target: α-AdrenoceptorXylometazoline is a nasal decongestant spray that constricts nasal blood vessels and increases nasal airflow, enabling patients with a blocked nose to breathe more easily. Xylometazoline is an effective and well-tolerated decongestant nasal spray that significantly relieved nasal congestion compared with placebo in the common cold and provided long-lasting relief with just 1 spray, helping patients to breathe more easily for a longer period of time [1]. Xylometazoline exhibited in radioligand competition studies higher affinities than the catecholamines adrenaline and noradrenaline at most α-adrenoceptor subtypes. Xylometazoline behaved at α(2B) -adrenoceptors as full agonists [2].
Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse[1][2].
Tamsulosin hydrochloride((R)-(-)-YM12617;LY253351) is a selective α1 receptor antagonist.Target: α1 receptorTamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B receptor in the blood vessels. Tamsulosin-treated patients had a 0.30-fold lower risk of developing acute urinary retention compared with control patients. None of the International Continence Society male questionnaire domain scores showed significant changes between the groups [1]. tamsulosin can be recommended for treating men after catheterization for AUR, and can reduce the likelihood of the need for re-catheterization [2].
Guanabenz is an orally active α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure[1].
Sertindole-d4 (Lu 23-174-d4) is the deuterium labeled Sertindole. Sertindole, a neuroleptic, is one of the newer antipsychotic medications available[1][2].
Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
KUL 7211 racemate is the racemate of KUL 7211. KUL 7211 is a selective β-adrenoceptor agonist.
Tetrahydrozoline is a potent α-adrenergic agonist and causes vasoconstriction. Tetrahydrozoline is used for the relief of conjunctival, ophthalmic and nasal congestion in vivo[1][2].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
(Rac)-Timolol-d5 Maleate ((Rac)-L-714,465-d5 Maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
MG 1 is an α1 adrenergic receptor antagonist.
Vemtoberant is an β3 Adrenergic Receptor antagonist. Vemtoberant can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure[1][2].
Carteolol HCl is a non-selective beta blocker used to treat glaucoma.Target: Beta adrenergic ReceptorCarteolol HCl is a beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. Carteolol hydrochloride at 1 mmol/L (P<0.05) significantly inhibited H2O2-induced cell damage and was able to scavenge O2 (EC50 value: 48 mmol/L). carteolol hydrochloride has a protective action against UVB-induced HCEC damage, and its radical scavenging ability may be an important basis for this effect [1]. The new alginate formulation of long-acting carteolol 1% given once daily is as effective as standard 1% carteolol given twice daily, with no meaningful differences regarding safety. This efficacy wasy was verified at 9 AM (24 hours after the last drop of long-acting carteolol or 12 hours after that of standard carteolol) and at 11 AM (2 hours after the morning drop). The new alginate formulation of long-acting carteolol 1% given once a day is effective and well tolerated by glaucoma patients who require chronic treatment [2].
Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist[1].
2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart[1][2].
Procaterol hydrochloride hemihydrate is an orally active β2 adrenoreceptor agonist. Procaterol hydrochloride hemihydrate can be used for the research of asthma[1][2][3].
Adrenalone hydrochloride is a selective α1-adrenoceptor agonist, used as a topical vasoconstrictor and hemostatic, used to prolong the action of local anesthetics.