Adrenergic Receptor

<p>Pronethalol ((±)-Pronethalol), a non-selective β-adrenergic antagonist, effectively inhibits Sox2 expression and offers protection against Digitalis-induced ventricular arrhythmias. Additionally, it can reverse such arrhythmias and limit the development of cerebral arteriovenous malformations (AVMs) [1] [2].</p>

<p>SDZ-NVI-085 is an α1 adrenergic receptor agonist and a competitive antagonist of 5-hydroxytryptamine.</p>

<p>Lidamidine (Lidamidinum) is an effective antidiarrheal agent that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle</p>

<p>Ro-70-0004 is a selective antagonist of alpha1A-adrenoceptor.</p>

<p>Ritobegron is used as a selective β3-adrenoceptor agonist and the prodrug of the active compound, KUC-7322.</p>

<p>Vemtoberant is a β3 adrenergic antagonist used in β3-related disorder research like heart failure.</p>

<p>Phentolamine Analogue 1 is an analogue of phentolamine. Phentolamine is a nonselective antagonist of α-adrenergic.</p>

<p>Bufuralol (Ro 3-4787) is a 尾-adrenergic receptor blocker with a certain degree of sympathomimetic effects and can be used to study cardiovascular diseases.</p>

<p>GW-597901, an β2 adrenergic receptor agonist, is used potentially for the treatment of asthma and chronic obstructive.</p>

<p>Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.</p>

<p>0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP</p>

<p>α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action.</p>

<p>OPC-28326: an α2-adrenergic blocker; dilates blood vessels; inhibits α2A/B/C receptors with Ki 2040/285/55 nM.</p>

<p>CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.</p>

<p>(±)-Prenalterol (H 80/62) is an agonist of beta-2- and beta-1-adrenergic receptors and is used to study chronic congestive heart failure.</p>

<p>Talibegron hydrochloride: β3 adrenoceptor agonist, pD2 3.72, relaxes rat arteries, reduces leptin in mice.</p>

<p>Deriglidole (SL 86-0715), an alpha2 receptor inhibitor, blocks colistin/Idazoxan but not prazosin/α2-adrenergic receptors.</p>

<p>(±)-Penbutolol ((Rac)-Penbutolol) is the racemic form of Penbutolol. It acts as an orally active β-adrenergic receptor antagonist. (±)-Penbutolol mitigates the tachycardia induced by exercise, reduces the increase in peak expiratory flow rate (PEFR) caused by physical activity, and decreases plasma renin activity (PRA) at rest. The peak plasma concentration of this compound is achieved one hour after oral administration, with a half-life of 4.5 hours, and it is metabolized into active metabolites in the body. This compound is utilized in research related to cardiovascular diseases.</p>

<p>TAAR1 agonist 3 is a potent agonist of Trace Amine-Associated Receptor 1 (TAAR1) with a pEC50 value of 7.6. Additionally, it acts as a full agonist at the α2AR with a pEC50 of 6. TAAR1 agonist 3 is utilized in the research of neuropsychiatric disorders.</p>

<p>Teoprolol is a blocker of β-adrenergic receptor.</p>

<p>SAR-150640, a selective β3-adrenergic receptor agonist, prevents an increase in MMP activity and production observed after LPS stimulation or in cases of chorioamnionitis.</p>

<p>Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).</p>

<p>Nipradolol blocks alpha-1-adrenergic receptors, lowers IOP in rabbits, and reduces NA-induced muscle contraction and dog artery vasodilation.</p>

<p>(Rac)-Nebivolol, a racemic β1-adrenergic blocker (IC50=0.8 nM), has vasodilatory properties and mitigates ethanol-induced cardiac harm.</p>

<p>DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.</p>

<p>PF-9404C: S-S diastereoisomer, beta-blocker with vasodilation, boosts cyclic GMP in rat aorta cells from 3 to 53 pmol/mg protein.</p>

<p>Ersentilide, a benzamide derivative, functions as both a β1-adrenergic receptor antagonist and an Ikr blocker. It has demonstrated efficacy in animal models of cardiac arrhythmias.</p>

<p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>

<p>L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.</p>

<p>Bometolol Hydrochloride is a beta-adrenergic blocking compound used for the treatment of cardiovascular disease.</p>

<p>LK-11, an alkaloid derivative, inhibits the passive uptake of norepinephrine (NA) by synaptic vesicles in the thalamus, similarly to cocaine.</p>

<p>Aclidinium, a dual-action compound, serves as a long-acting muscarinic antagonist and a β2-adrenoceptor (β2-AR) agonist, exhibiting bronchodilator properties. It effectively reduces lung hyperinflation, enhances lung function, and prolongs exercise endurance time. This compound is commonly utilized in studies focusing on chronic obstructive pulmonary disease (COPD).</p>

<p>BRL-37344 is a selective β3-adrenergic receptor agonist. It significantly reduces the body weight of obese mice.</p>

<p>Mafoprazine, a phenylpiperazine derivative, exhibits varying affinities for neuronal receptors, primarily exerting its antipsychotic effects through blocking D2 receptors and enhancing α-adrenergic activity. It also increases the activity of dopamine metabolites.</p>

<p>RU 52583 is an alpha 2-adrenergic receptor antagonist.</p>

<p>AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.</p>

<p>(S)-Bucindolol is an enantiomer of bucindolol, specifically a β1-adrenergic receptor antagonist. It is primarily utilized in research related to heart failure.</p>

<p>Butopamine hydrochloride is an orally active inotropic compound that is more effective at increasing heart rate compared to Dobutamine.</p>

<p>Sulfinalol hydrochloride is an orally active β-adrenoceptor (β-adrenoceptor) antagonist that exhibits direct vasodilatory activity. It is also classified as an antihypertensive agent.</p>

<p>Metipranolol hydrochloride is a non-selective β-adrenergic receptor blocking agent.</p>

<p>HOKU-81is a new bronchodilator and is one of the metabolites of tulobuterol.</p>

<p>Atenolol (Tenormin) is a selective β1 receptor antagonist.</p>

<p>Picumeterol(GR 114297A) is a potent and selective β2 adrenergic receptor agonist. In vitro and in vivo trials, Picumeterol produced long-lasting airway smooth muscle relaxation. Picumeterol is a pure R enantiomer that can be used to improve lung function and reduce airway hyperreactivity in patients with asthma.</p>

<p>4-Hydroxyatomoxetine, an active metabolite of Atomoxetine, is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.</p>

<p>4-Hydroxypropranolol hydrochloride is an active metabolite of Propranolol, with a potency comparable to Propranolol. It inhibits β1- and β2-adrenergic receptors (pA2s: 8.24 and 8.26).</p>