Adrenergic Receptor

<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>N-5984, a β3-adrenergic receptor agonist, is used potentially for the treatment of obesity, overactive bladder and type 2 diabetes.</p>

<p>4-Hydroxy Nebivolol, a primary metabolite of Nebivolol, results from the enzymatic hydroxylation of Nebivolol by the cytochrome P450 (CYP) isoform CYP2D6.</p>

<p>(-)-Isoproterenol hydrochloride is used as a β-adrenergic receptor agonist in the treatment of bradycardia and as a bronchodilator.</p>

<p>BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR, Kd of 84 pM).</p>

<p>AGN 192836 is a potent and selective α2 adrenergic agonist (EC50s: 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor).</p>

<p>β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).</p>

<p>Todralazine hydrochloride, a β2AR blocker with antioxidant properties, is used in hypertension studies.</p>

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity.

<p>Bunazosin Hydrochloride (E 1015) is an alpha(1)-adrenoceptor antagonist used as a systemic antihypertensive and an ocular hypotensive drug.</p>

<p>RS 17053 hydrochloride: selective α1A adrenoceptor antagonist, pKi 9.1, pA2 9.8.</p>

<p>AR-08 is a potent α2-adrenergic receptor agonist for the study of ADHD and attention deficit.</p>

<p>Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.</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>Talibegron hydrochloride: β3 adrenoceptor agonist, pD2 3.72, relaxes rat arteries, reduces leptin in mice.</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>Deriglidole (SL 86-0715), an alpha2 receptor inhibitor, blocks colistin/Idazoxan but not prazosin/α2-adrenergic receptors.</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>Teoprolol is a blocker of β-adrenergic receptor.</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>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>(Rac)-Nebivolol, a racemic β1-adrenergic blocker (IC50=0.8 nM), has vasodilatory properties and mitigates ethanol-induced cardiac harm.</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>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>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>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</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>Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).</p>

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

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

<p>Nipradolol blocks alpha-1-adrenergic receptors, lowers IOP in rabbits, and reduces NA-induced muscle contraction and dog artery vasodilation.</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>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>AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.</p>

<p>RU 52583 is an alpha 2-adrenergic receptor antagonist.</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>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>Butopamine hydrochloride is an orally active inotropic compound that is more effective at increasing heart rate compared to Dobutamine.</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>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>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>4-Hydroxyatomoxetine, an active metabolite of Atomoxetine, is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.</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-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>