α-adrenergic receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1283 Asenapine

Asenapine is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

Selective α2C-adrenergic receptor, pKi: 8.91; α2B-adrenergic receptor, pKi: 9.49; α1A-adrenergic receptor, pKi: 8.93; α2A-adrenergic receptor, pKi: 8.9
S4266 Brimonidine Tartrate

Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.

Selective α2a-adrenergic receptor, EC50: 0.45 nM
S3075 Dexmedetomidine

Dexmedetomidine is a sedative medication used by intensive care units and anesthetists.

Selective α2 receptor, Ki : 1.08 nM
S3060 Medetomidine HCl

Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Selective α2-adrenoceptor, Ki: 1.08 nM
S4065 Guanabenz Acetate

Guanabenz Acetate is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.

Selective α2c-adrenergic receptor, pEC50: <5; α2b-adrenergic receptor, pEC50: 7.01; α2a-adrenergic receptor, pEC50: 8.25
S2126 Naftopidil

Naftopidil is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM.

Selective α1-adrenergic receptor, Ki: 58.3 nM
S2576 Xylometazoline HCl

Xylometazoline is an α-adrenoceptor agonist commonly used as nasal decongestant, exhibits highest potency at α2B-adrenoceptor subtype with EC50 of 99 μM.

Selective adrenoceptor α1D, IC50: 450 nM; adrenoceptor α2A, IC50: 980 nM; adrenoceptor α2A, IC50: 980 nM; adrenoceptor α2B, IC50: 1800 nM; adrenoceptor α2C, IC50: 220 nM; adrenoceptor α1B, IC50: 560 nM; adrenoceptor α1A, IC50: 80 nM
S2038 Phentolamine Mesylate

Phentolamine Mesylate is a nonselective alpha-adrenergic antagonist with IC50 of 0.1 μM.

Selective α-adrenergic receptor, IC50: 100 nM
S1387 Naftopidil DiHCl

Naftopidil DiHCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

Selective α1-adrenergic receptor, IC50: 0.2 μM
S2569 Phenylephrine HCl

Phenylephrine HCl is a selective α1-adrenergic receptor agonist.

Selective
S2545 Scopine

Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.

Selective
S1642 Methyldopa

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.

Selective
S1613 Silodosin

Silodosin is an α1-adrenoceptor antagonist with high uroselectivity.

Selective
S2499 Phenoxybenzamine HCl

Phenoxybenzamine HCl is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM.

Selective
S1409 Alfuzosin HCl

Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).

Selective
S1324 Doxazosin Mesylate

Doxazosin, a quinazoline-derivative, selectively antagonizes postsynaptic α1-adrenergic receptors, used in the treatment of high blood pressure and urinary retention associated with benign prostatic hyperplasia.

Selective
S4124 Tolazoline HCl

Tolazoline is a non-selective competitive α-adrenergic receptor antagonist.

Selective
S2059 Terazosin HCl

Terazosin HCl is an alpha-adrenergic blocker used to treat high blood pressure and enlarged prostate.

Selective
S3185 Adrenalone HCl

Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.

Selective
S2458 Clonidine HCl

Clonidine HCl is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.

Selective
S2373 Yohimbine HCl

Yohimbine has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac.

Selective
S1437 Tizanidine HCl

Tizanidine HCl is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

Selective
S1424 Prazosin HCl

Prazosin HCl, a quinazoline derivative, is the first of a new chemical class of antihypertensives.

Selective
S2438 Synephrine HCl

SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist.

Selective
S2516 Xylazine HCl

Xylazine is an α2-Adrenergic receptor agonist, used as a sedative and muscle relaxant.

Selective
S2090 Dexmedetomidine HCl

Dexmedetomidine HCl is a highly selective and potent alpha-2 adrenoceptor agonist, which reduces anesthetic requirements for patients by providing significant sedation.

Selective
S4043 Tetrahydrozoline HCl

Tetrahydrozoline HCl is an imidazoline derivative with alpha receptor agonist activity.

Selective
S2615 Noradrenaline bitartrate monohydrate

Noradrenaline bitartrate monohydrate is a direct alpha-adrenergic receptors stimulator.

Selective
S2691 BMY 7378 Dihydrochloride

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

Pan α2-adrenoceptor, pIC50: 5.1; α1D-adrenoceptor, pKi: 8.2; α2C-adrenoceptor, pKi: 6.54
S4291 Labetalol HCl

Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors, used in the treatment of high blood pressure.

Pan
S1831 Carvedilol

Carvedilol is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.

Pan
S2521 Epinephrine Bitartrate

Epinephrine Bitartrate is an alpha- and beta-adrenergic receptor stimulator.

Pan