α-adrenergic receptor Selective Inhibitors | Agonists | Antagonists

N° de cat.	Nom du produit	Informations	Sélectif / 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
S3060	Medetomidine HCl	Medetomidine is a selective α2-adrenoceptor agonist, with K_i 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 α_2B-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	BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pK_i of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pK_i 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

α-adrenergic receptor-Sélectif Inhibitors | Agonists | Antagonists