Adrenergic Receptor Antagonist

Propranolol is a nonselective and BBB-permeable β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

Propranolol hydrochloride is a nonselective and BBB-permeableβ-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a K_i of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.

Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.

Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.

Pimozide is a dopamine receptor antagonist, with K_is 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 K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5.

Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively.

Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research.

Prazosin is an α-adrenergic receptor antagonist. Prazosin can reduce inflammation, relieve anxiety, alleviate panic, prevent memory decline, and modulate the pain-relieving effects of opioids. Prazosin can be used in the study of hypertension and Alzheimer’s disease.

Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with K_i values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.

(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.

Labetalol (AH5158) is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.

SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

Phentolamine is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine reduces systemic vascular resistance and increases cardiac output. Phentolamine improves erectile dysfunction. Phentolamine can be used for the research of erectile dysfunction.

Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (K_i=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with K_i values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.

Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.

Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

Pindolol (LB-46) is the antagonist for 5-HT 1A (K_i=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects.