Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor[1].
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.
Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research[1][2].
Naphazoline HCl is an ocular vasoconstrictor and imidazoline derivative sympathomimetic amine.Target: Adrenergic Receptorphazoline hydrochloride is the common name for 2-(1-naphthylmethyl)-2-imidazoline hydrochloride. It is a sympathomimetic agent with marked alpha adrenergic activity. It is a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane. It acts on alpha-receptors in the arterioles of the conjunctiva to produce constriction, resulting in decreased congestion. It is an active ingredient in several over-the-counter formulations including Clear Eyes and Naphcon eye drops. From Wikipedia.
Romifidine is an α2 adrenergic receptor agonist. Romifidine shows sedation effects in vivo[1][2].
Pronethalol is a non-selective beta-adrenergic blocking agent, protect against and to reverse Digitalis-induced ventricular arrhythmias. Target: beta-adrenergic receptor
Moxisylyte (hydrochloride) is (alpha 1-blocker) antagonist，it can vasodilates cerebral vessels without reducing blood pressure。It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. [1][2]
Clorprenaline is a potent agonist of β2-adrenergic. Clorprenaline promotes animal muscular mass growth and decreases fat accumulation. Clorprenaline is a potential new lean meat-boosting feed additive[1].
Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity[1].
Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia, cocaine addition, and obesity[1][3].
3-Hydroxy-4-methoxycinnamic acid (Isoferulic acid) is a cinnamic acid derivative that has antidiabetic activity. 3-Hydroxy-4-methoxycinnamic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use.
Doxazosin(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.Target: Adrenergic ReceptorDoxazosin is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms [1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor, thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium [2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%), and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy [3].Clinical indications: Hypertension; Prostate hyperplasiaFDA Approved Date: February 22, 2005Toxicity: Symptoms of overdose include hypotension
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
Guanfacine is a selective α2A receptor agonist.Target: α2A ReceptorGuanfacine is a sympatholytic. It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone [1, 2].
Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors[1].
Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
(±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist[1].
Vibegron (MK-4618) is a potent, highly selective β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder[1][2][3].
Tetrahydrozoline (hydrochloride) is a α-adrenoceptor agonist. Target: α-adrenoceptorahydrozoline is an imidazoline derivative with alpha receptor agonist activity widely available in over-the-counter topical ocular and nasal formulations. More than 1,600 cases of oral exposures are reported to United States poison centers annually (1,2). Reports of significant toxicity from tetrahydrozoline ingestion are unusual but have occured primarily in small children after unintentional ingestion (3-63, 6) [1].
Norepinephrine bitartrate monohydrate is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
Guanfacine Hcl, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. IC50 Value: 31 nM(Kd)Target: Adrenergic ReceptorGuanfacine is a sympatholytic. It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone. From Wikipedia
CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors[1].
Terazosin Hydrochloride dihydrate is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin Hydrochloride dihydrate is an a1-selective blocker. Its inhibitory effect on prostate tumor growth may be the result of antiangiogenic activity. Terazosin Hydrochloride dihydrate is an inhibitor of α1A-AR, α1B-AR, α1D-AR and α2B-AR [1].
Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
Butyryltimolol, an effective prodrug of Timolol, improves the corneal penetration of Timolol[1]. Butyryltimolol is a β-adrenergic blocker[2].
Phenoxybenzamine hydrochloride is a selective antagonist of both α-adrenoceptor and calmodulin that is commonly used for the treatment of hypertension, specifically caused by pheochromocytoma.
Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder)[1][2][3][4].
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.
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.