α-adrenergic receptor Selective Inhibitors | Agonists | Antagonists

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S5537	Tizanidine	Tizanidine is an imidazoline derivative and a centrally acting α2 adrenergic agonist used as a muscle relaxant for therapy of acute muscle spasms and chronic spasticity.	Selective
S4649	Atipamezole hydrochloride	Atipamezole (Antisedan, MPV1248) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride is hydrochloride form of atipamezole.	Selective
S5954	L-(-)-α-Methyldopa hydrate	L-(-)-α-Methyldopa (Methyldopa, MK-351) hydrate, a potent antihypertensive drug, is a selective agonist for α2-adrenergic receptors.	Selective
S6345	3-Nitro-L-tyrosine	3-Nitro-L-tyrosine (3-NT, N-Tyr, MNT), synthesized from L-tyrosine by peroxynitrite, is a product of nitric oxide and superoxide. 3-Nitro-L-tyrosine inhibits the hemodynamic responses to angiotensin II, possibly through the inhibition of alpha 1-adrenoceptor-mediated events.	Selective
S4650	Atipamezole	Atipamezole (MPV-1248, MPV1248, Antisedan) is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug.	Selective
S4797	Nicergoline	Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.	Selective
S5965	Urapidil	Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.	Selective
S4693	Guanfacine Hydrochloride	Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.	Selective
S5780	Prazosin	Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors. It is used to treat hypertension.	Selective
S0116	Piperoxan hydrochloride	Piperoxan hydrochloride (Benodaine, Fourneau 933, F933, DL-Piperoxan) is an antagonist of α2 (alpha 2) adrenoceptor.	Selective
S4481	Guanabenz	Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.	Selective
S1283	Asenapine maleate	Asenapine maleate (Org 5222) 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	α1A-adrenergic receptor, pKi: 8.93; α2A-adrenergic receptor, pKi: 8.9; α2B-adrenergic receptor, pKi: 9.49; α2C-adrenergic receptor, pKi: 8.91
S4266	Brimonidine Tartrate	Brimonidine Tartrate(UK 1434 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
S2126	Naftopidil	Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with K_i of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.	Selective	α1A-adrenergic receptor, Ki: 3.7 nM; α1B-adrenergic receptor, Ki: 20 nM; α1D-adrenergic receptor, Ki: 1.2 nM
S0862	L-765314	L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.	Selective	α1b-adrenoceptor, IC50: 1.9 nM; α1b-adrenoceptor, Ki: 5.4 μM; α1b-adrenoceptor, Ki: 2 μM
S4065	Guanabenz Acetate	Guanabenz Acetate (WY-8678) 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	α2a-adrenergic receptor, pEC50: 8.25; α2b-adrenergic receptor, pEC50: 7.01; α2c-adrenergic receptor, pEC50: <5
S5337	Rauwolscine hydrochloride	Rauwolscine hydrochloride (Isoyohimbine, α-Yohimbine, corynanthidine) is the hydrochloride salt form of Rauwolscine, a specific and potent α2 antagonist with Ki of 12 nM.	Selective	α2 adrenergic receptor, Ki: 12 nM
S3913	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.	Selective	Adrenergic α-1A, pKi: 7.61
S4358	Pimozide	Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.	Selective	α1-adrenoceptor, Ki: 39 nM
S3656	Piribedil	Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.	Selective	adrenoceptor α2A, pKi: 7.1; adrenoceptor α2C, pKi: 7.2
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 α1A, IC50: 80 nM; adrenoceptor α1B, IC50: 560 nM; 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
S1387	Naftopidil DiHCl	Naftopidil DiHCl (Flivas, KT-611, Avishot,BM-15275) 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
S2516	Xylazine HCl	Xylazine(BAY 1470 hydrochloride) is an α2-Adrenergic receptor agonist, used as a sedative and muscle relaxant.	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(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.	Selective
S2059	Terazosin HCl Dihydrate	Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).	Selective
S1424	Prazosin HCl	Prazosin HCl (cp-12299-1) is a competitive alpha-1 adrenoceptor antagonist, used to treat high blood pressure or benign prostatic hyperplasia.	Selective
S1613	Silodosin	Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.	Selective
S1437	Tizanidine HCl	Tizanidine HCl (DS 103-282) is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.	Selective
S2373	Yohimbine HCl	Yohimbine (Antagonil) has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac.	Selective
S4043	Tetrahydrozoline HCl	Tetrahydrozoline (Tetryzoline) HCl is an imidazoline derivative with alpha receptor agonist activity.	Selective
S2615	Noradrenaline bitartrate monohydrate	Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.	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
S2569	Phenylephrine (NCI-C55641) HCl	Phenylephrine HCl (NCI-c55641,Phenylephrine hydrochloride,(R)-(-)-Phenylephrine hydrochloride, L-Phenylephrine hydrochloride) is a selective α1-adrenergic receptor agonist, used primarily as a decongestant.	Selective
S4124	Tolazoline HCl	Tolazoline(Imidaline hydrochloride,NSC35110 hydrochloride) is a non-selective competitive α-adrenergic receptor antagonist.	Selective
S1409	Alfuzosin HCl	Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).	Selective
S2499	Phenoxybenzamine HCl	Phenoxybenzamine HCl (NSC 37448, NCI-c01661) is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM.	Selective
S2038	Phentolamine Mesylate	Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes.	Selective
S2090	Dexmedetomidine HCl	Dexmedetomidine HCl((+)-Medetomidine Hydrochloride) is a highly selective and potent alpha-2 adrenoceptor agonist, which reduces anesthetic requirements for patients by providing significant sedation.	Selective
S2545	Scopine	Scopine(6,7-Epoxytropine) is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.	Selective
S2438	Synephrine HCl	SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist.	Selective
S2691	BMY 7378 Dihydrochloride	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	α2C-adrenoceptor, pKi: 6.54; α1D-adrenoceptor, pKi: 8.2; α2-adrenoceptor, pIC50: 5.1
S9507	(−)-Norepinephrine	(−)-Norepinephrine (Arterenol, Levarterenol, L-Noradrenaline) is a natural neurotransmitter and hormone. It is an agonist of adrenergic receptors with Ki values of 330, 56, and 740 nM for α1, α2, and β1 adrenoceptors, respectively.	Pan	α1 adrenoceptor, Ki: 330 nM; α2A adrenoceptor, Ki: 56 nM
S1831	Carvedilol	Carvedilol (BM-14190, SKF 105517) is a non-selective beta blocker/alpha-1 blocker, used to treat congestive heart failure (CHF) and high blood pressure.	Pan
S3960	Higenamine hydrochloride	Higenamine (Norcoclaurine, (+-)-Demethylcoclaurine), also known as Norcoclaurine HCl, is a non-selective β2 adrenoceptor agonist which is a chemical compound naturally occurring in a number of plants.	Pan
S4291	Labetalol HCl	Labetalol HCl(AH-5158 hydrochloride,Labetalol hydrochloride,Sch-15719W) is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors, used in the treatment of high blood pressure.	Pan
S2521	Epinephrine bitartrate	Epinephrine bitartrate (Adrenalinium) is an alpha- and beta-adrenergic receptor stimulator.	Pan