Adrenergic Receptor

Bedoradrine sulfate (MN-221 sulfate) is a super-selective beta2 agonist for the treatment of asthma exacerbations and chronic obstructive pulmonary disease.

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting antagonist of 5-HT2 receptor (IC50: 0.9 nM), less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

Bedoradrine free base is a novel, highly selective β2-adrenoceptor agonist for the treatment of asthma and chronic obstructive pulmonary disease (COPD).

CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.

AVN-101 is a potent 5-HT7 receptor antagonist.

Terbutaline is a short-acting agonist of β2-adrenergic receptor (β2-AR) . It is an active metabolite of bambuterol

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Dexmedetomidine hydrochloride (Precedex) is an imidazole derivative that is an agonist of the adrenergic alpha-2 receptor. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

Alfuzosin (SL 77499) is an orally available, competitive α1-adrenoceptor antagonist.Alfuzosin induces smooth muscle relaxation in the bladder neck and prostate.Alfuzosin has been used to study benign prostatic hypertrophy, lower urinary tract symptoms (LUTS), and ejaculatory dysfunction (EjD).

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

Buflomedil hydrochloride (Fonzylane), a vasodilator, is used in therapy of claudication or the symptoms of the peripheral arterial disease.

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.

Gramine (Donaxine), a natural indole alkaloid, present in several plant species, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine has anti-tumor, anti-viral and anti-inflammatory properties.

Adrenalone hydrochloride (Adrenalone HCl) is a dopamine β-oxidase inhibitor with a similar structure to the norepinephrine transporter (NET) ligand, with an IC50 of 36.9 μM. It is an adrenergic agonist that acts as a local vasoconstrictor and hemostatic agent.

Butofilolol is a novel beta-blocker with antihypertensive activity and can be used to study hypertension.

RS 17053 hydrochloride is a potent and selective antagonist of α1A adrenoceptor. RS 17053 hydrochloride exhibits a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

Tamsulosin hydrochloride (Flomax hydrochloride) is the hydrochloride salt of tamsulosin, a sulfonamide derivative with α1 adrenergic antagonist activity.

Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.

MG 1 is a potent alpha-1 adrenergic receptor antagonist.

Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

RS 15385-198 is a less active isomer of Delequamine. Delequamine is a selective alpha2-adrenergic receptor antagonist.

OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.

Esprolol (ACC-9369 free base) is a novel β-adrenergic receptor antagonist for the study of exertional angina.

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

ACTH 1-14 acetate(25696-21-3 free base) (Adrenocorticotropic Hormone Fragment 1-14 acetate) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.Adrenocorticotropic hormone (ACTH), also known as corticotropin, is produced and secreted by the anterior pituitary gland. ACTH is an important component of the hypothalamic-pituitary-adrenal axis as a response to biological stress.

T-0509 is a selective beta 1 receptor agonist that increases inotropy in canine ventricular muscle and selectively down-regulates rat cardiac beta 1-adrenoceptors.

Taprizosin（UK-338003） is a selective and orally active α1-adrenoceptor antagonist for vasodilatation in the treatment of benign prostatic hyperplasia.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist that shows antihypertensive and antiplatelet aggregation activity in hypertensive rats.

Nardeterol HCl is a β-adrenergic receptor partial agonist used in the study of the central nervous system.CAS 번호13460-73-83-4

(S)-(+)-Niguldipine hydrochloride is a selective α1A-AR antagonist used in the study of depression and epilepsy.

Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction as a result of overdose with certain 5-HT2A agonist drugs.

LUN42518 HCl is an analogue of phentolamine. Phentolamine is a nonselective alpha-adrenergic antagonist.

(S)-(-)-Atenolol has beta-adrenergic blocking effects.

Palatrigine (BW-A 256C) is a compound with angiotensin-converting enzyme inhibitory and beta-adrenergic receptor blocking properties.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

Imiloxan (RS-21361) is an α2 adrenergic receptor antagonist used in the treatment of major depressive disorder.

Dabelotine (UNII-6RY56RB98P) is an adrenergic agonist used in the study of dementia.

Neldazosin is used as a potent α1-adrenoceptor antagonist.

N-methyltyramine is an alkaloid isolated from the leguminous plant Acacia grandiflora.It is an α2-adrenoceptor antagonist that regulates adrenergic receptors through enzymatic adrenergic synthesis.It is used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.

Tolnapersine TFA is a mixed dopamine agonist and alpha adrenergic receptor antagonist.

Tienoxolol FA is a small molecule beta-adrenergic receptor antagonist used in the treatment of cardiovascular disease and in the study of hypertension and cardiac machine ischemia.

TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.