• α-adrenergic receptor
  • β-adrenergic receptor

α-adrenergic receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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
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
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
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
S4693 Guanfacine Hydrochloride Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect. Selective
S3643 Amitraz Amitraz (NSC 324552) is a triazapentadiene, an α2 adrenergic agonist and a member of the amidine chemical family. It is a non-systemic acaricide and insecticide. 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 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
S2126 Naftopidil Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with Ki 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 α1D-adrenergic receptor, Ki: 1.2 nM; α1B-adrenergic receptor, Ki: 20 nM; α1A-adrenergic receptor, Ki: 3.7 nM
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 α2c-adrenergic receptor, pEC50: <5; α2a-adrenergic receptor, pEC50: 8.25; α2b-adrenergic receptor, pEC50: 7.01
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
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 α2B-adrenoceptor subtype with EC50 of 99 μM. Selective adrenoceptor α2C, IC50: 220 nM; adrenoceptor α2B, IC50: 1800 nM; adrenoceptor α2A, IC50: 980 nM; adrenoceptor α2A, IC50: 980 nM; adrenoceptor α1A, IC50: 80 nM; adrenoceptor α1B, IC50: 560 nM; adrenoceptor α1D, IC50: 450 nM
S1387 Naftopidil DiHCl Naftopidil DiHCl (KT-611) 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
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 α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. Selective α2-adrenoceptor, Ki: 360 nM
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
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
S5965 Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist. Selective
S2499 Phenoxybenzamine HCl Phenoxybenzamine HCl (NSC 37448, NCI-c01661) is a non-specific, irreversible alpha antagonist with an IC50 of 550 nM. 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
S2516 Xylazine HCl Xylazine is an α2-Adrenergic receptor agonist, used as a sedative and muscle relaxant. Selective
S4481 Guanabenz Guanabenz (GBZ, GA, Wytensin, Wy-8678) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action. Selective
S4043 Tetrahydrozoline HCl Tetrahydrozoline (Tetryzoline) HCl is an imidazoline derivative with alpha receptor agonist activity. Selective
S2038 Phentolamine Mesylate Phentolamine Mesylate is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes. 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
S2059 Terazosin HCl Dihydrate Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH). Selective
S3185 Adrenalone HCl Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. 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
S1409 Alfuzosin HCl Alfuzosin HCl is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). 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
S2458 Clonidine HCl Clonidine HCl is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg. 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
S2438 Synephrine HCl SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist. Selective
S0116 Piperoxan hydrochloride Piperoxan hydrochloride (Benodaine, Fourneau 933, F933, DL-Piperoxan) is an antagonist of α2 (alpha 2) adrenoceptor. Selective
S4124 Tolazoline HCl Tolazoline is a non-selective competitive α-adrenergic receptor antagonist. Selective
S2569 Phenylephrine (NCI-C55641) HCl Phenylephrine HCl (NCI-C55641) is a selective α1-adrenergic receptor agonist, used primarily as a decongestant. 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
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
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; α2C-adrenoceptor, pKi: 6.54; α1D-adrenoceptor, pKi: 8.2
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
S2521 Epinephrine bitartrate Epinephrine bitartrate (Adrenalinium) is an alpha- and beta-adrenergic receptor stimulator. 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
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
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