| 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 |
|
| 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 |
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 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 |
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 α2B-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 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 |
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 |
|
