α1-adrenergic receptor

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

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

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

Aplindore Fumarate (DAB-452) is a small molecule dopamine D2 receptor partial agonist.Aplindore Fumarate exhibits high affinity for dopamine D2 and D3 receptors, and low affinity for dopamine D4, 5-hydroxytryptophan (5-HT2), and α1-adrenergic receptors.Aplindore Fumarate is used in the study of Parkinson's disease and schizophrenia. Fumarate can be used to study Parkinson's and schizophrenia.

SM-2470 is an α1-adrenoceptor antagonist with antihypertensive activity that decreases anterior ganglionic adrenal nerve activity and aortic descending nerve activity.SM-2470 has hypocholesterolemic activity and inhibits cholesterol absorption.

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

Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.

Labetalol hydrochloride (Sch-15719W), a salicylamide derivative, is a non-cardioselective blocker of β-adrenergic receptors and α1-adrenergic receptors.

Phenylephrine hydrochloride (NCI-c55641) is a selective agonist of the α1-adrenergic receptor.

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.

Scopine (6,7-Epoxytropine), the metabolite of anisodine, is an α1-adrenergic receptor agonist used in the therapy of acute circulatory shock.

BMY-14802 hydrochloride (BMS 181100 hydrochloride) is a selective antagonist of σ receptor (IC50 = 112 nM) with antipsychotic effects. BMY-14802 hydrochloride is an agonist of the α1-adrenergic receptor and 5-HT1A.

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.

Lidanserin is an antagonist of the 5-HT2A and α1-adrenergic receptor.

Midodrine is converted to its active metabolite, desglymidodrine by deglycination reaction. Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. This causes smooth muscle contraction and leads to an elevation of blood pressure. Desglymidodrine diffuses poorly across the blood-brain barrier and is therefore not associated with effects on the central nervous system. Midodrine hydrochloride (Pro-Amatine) is the hydrochloride salt form of midodrine, a direct-acting prodrug and sympathomimetic agent with antihypotensive properties.

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic, and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM, and 8 nM, respectively. This second-generation antipsychotic is primarily used to treat schizophrenia, and clinical trials have investigated its efficacy as an antimanic agent in patients with acute bipolar mania.

Doxazosin (UK 33274) is a long-acting α1-adrenoceptor inhibitor widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms.

Prazosin (Prazosine), an α1-blocker, acts as an inverse agonist at alpha-1 adrenergic receptors and is used to treat hypertension.

Dapiprazole Hydrochloride (Glamidolo Hydrochloride) is an alpha-1-adrenergic antagonist that acts by blocking alpha-adrenergic receptors in the smooth muscle of blood vessels (arteries, arterioles and veins), gastrointestinal tract, and radial smooth muscle of the iris.

Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

Scopine hydrochloride (6,7-Epoxytropine hydrochloride), a metabolite of anisodine, acts as an α1-adrenergic receptor agonist and is utilized in managing acute circulatory shock.