α adrenergic receptor Antagonist

Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.

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.

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.

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.

Atipamezole (MPV 1248) is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM.

Atipamezole (MPV-1248) hydrochloride is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM.

Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT₂, 5-HT₃, histamine H1 receptor and α2-adrenoceptor antagonist with pK_i values of 8.05, 8.1, 9.3 and 6.95, respectively.

Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.

Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.

Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is 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 (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.

BMY 7378 is a selective antagonist of α_1D-adrenoceptor (α_1D-AR). BMY 7378 binds to membranes expressing the cloned rat α_1D-AR with a >100-fold higher affinity (K_i=2 nM) than binding to either the cloned rat α_1A-AR (K_i=800 nM) or the hamster α_1B-AR (K_i=600 nM). BMY 7378 is a 5-HT_1A receptor partial agonist.

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

Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.

Doxazosin mesylate (UK 33274 mesylate) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.

Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.

Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (K_i=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC₅₀ of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.

Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.

JP1302 dihydrochloride is a potent, selective, high affinity antagonist of the α_2C-adrenoceptor, with a K_b of 16 nM and a K_i of 28 nM for the human α_2C-receptor. JP1302 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research.