adrenoceptor antagonist

RS 17053 hydrochloride is a potent and selective antagonist of α1A adrenoceptor. RS 17053 hydrochloride exhibits a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

Taprizosin（UK-338003） is a selective and orally active α1-adrenoceptor antagonist for vasodilatation in the treatment of benign prostatic hyperplasia.

Neldazosin is used as a potent α1-adrenoceptor antagonist.

N-methyltyramine is an alkaloid isolated from the leguminous plant Acacia grandiflora.It is an α2-adrenoceptor antagonist that regulates adrenergic receptors through enzymatic adrenergic synthesis.It is used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.

Bunazosin Hydrochloride (E 1015) is an alpha(1)-adrenoceptor antagonist used as a systemic antihypertensive and an ocular hypotensive drug.

Cicloprolol hydrochloride is a new potent and selective beta 1-adrenoceptor antagonist with partial agonist activity for the study of coronary heart disease.

SM-2470 is an α1-adrenoceptor antagonist with antihypertensive activity that decreases anterior ganglionic adrenal nerve activity and aortic descending nerve activity.SM-2470 has hypocholesterolemic activity and inhibits cholesterol absorption.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

ORM-10921 is an α2C-adrenoceptor antagonist that has shown antipsychotic and antidepressant activity in animal studies.

Fluparoxan hydrochloride is a highly selective and potent α2-adrenoceptor antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist, has weak α1 adrenoceptor blocking activity.

CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

Midaglizole ((±)-DG5128 free base, DG5128 free base) is a powerful α2-adrenoceptor antagonist that acts as a hypoglycemic agent by increasing blood pressure and lowering blood glucose levels in vivo.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

Bupranolol is an antagonist of β2-adrenergic receptor and has been used for angina pectoris, hypertension, glaucoma, cardiac arrhythmia and as an antithrombotic.

Naftopidil dihydrochloride (KT-611 2HCl) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

Alpha-Yohimbine is a 5-HT1A receptor agonist, it is strong selective 2-adrenoceptor antagonist. Alpha-Yohimbine possess aphrodisiac effect.

LAS190792 (AZD8999) is a dual-action chemical compound that simultaneously acts as a strong muscarinic antagonist and β2-adrenoceptor agonist. It exhibits significant potency across a range of receptors, with pIC50 values of 8.9 for M1, 8.8 for M2, 8.8 for M3, 9.2 for M4, 8.2 for M5, 7.5 for β1, 9.1 for β2, and 5.6 for β3. Its effectiveness across these receptors makes LAS190792 a viable candidate for bronchodilator applications [1].

(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent antagonist of α1-adrenoceptor (α1a, α1b and α1d-adrenoceptor with Ki values of 6.51 nM, 1.01 nM and 1.97 nM, respectively).

Urapidil hydrochloride (Urapidil HCl) is 5-HT1A receptor agonist and an α1-adrenoceptor antagonist.

Dicentrine, a selective α±(1)-adrenoceptor antagonist with potent antiarrhythmic and antihypertensive activities, it also has antinociception in different models of chemical pain.

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor. It demonstrates a significant affinity for the β2 adrenoceptor, indicated by an EC50 value of 9.2 nM, and for the muscarinic receptor with a Ki value of 30.2 nM. Furthermore, its MABA activity is highlighted by an EC50 value of 4.0 nM [1].

R-(-)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker; potassium agonist that activates Ca2+-activated maxi K-channel; alpha1A-adrenoceptor antagonist; antihypertensive agent; Less active enantiomer.

Terazosin dimer impurity dihydrochloride, a dimeric form of Terazosin, is a chemical impurity found in Terazosin. Terazosin itself is a derivative of quinazoline and acts as a competitive and orally active α1-adrenoceptor antagonist[1].

Fiduxosin hydrochloride is an alpha 1a-adrenoceptor antagonist that may be useful in the treatment of Benign Prostatic Hyperplasia.

Bopindolol ((±)-Bopindolol) fumarate is an orally active β-adrenoceptor (ARs) antagonist with partial agonist activity that is non-selective for β1- and β2-ARs and has low affinity for the β3-AR subtype. Bopindolol fumarate is a precursor drug to Pindolol and can be used to study primary and renal vascular hypertension.

L-771688 is an α1A-adrenoceptor antagonist potentially for the treatment of benign prostatic hyperplasia.

Upidosin (SB-216469) is a potential uroselective α1-adrenoceptor antagonist, α1a subtype Ki=0.34 nM, α1b subtype Ki=3.9 nM, α1d subtype Ki=1.5 nM, α2-adrenoceptor Ki=33.3 nM.

β-adrenoceptor and 5-HT1A/1B receptor antagonist

BRL 44408 Maleate Salt is a selective α2A-adrenoceptor antagonist with Ki value of 1.7 nM. BRL 44408 Maleate Salt increases the release of hippocampal noradrenalin following systemic administration.

α2 adrenoceptor antagonist and imidazoline I1 receptor ligand

Amosulalol is a combined alpha and beta adrenoceptor antagonist.

SKF 86466 hydrochloride is an α2-adrenoceptor antagonist.

5-Methylurapidil is an alpha1A-adrenoceptor antagonist.

Abanoquil is an antagonist of alpha-1 adrenoceptor.

ORM-13070 is a selective antagonist radioligand for the α2C adrenoceptor subtype. ORM-13070 C-11 is under investigation in clinical trial.

Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).

Acepromazine-d6 maleate is a deuterated compound of Acepromazine maleate. Acepromazine maleate has a CAS number of 3598-37-6. ACEPROMAZINE MALEATE is a dopamine receptor antagonist

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

HEAT hydrochloride is an α1-adrenoceptor antagonist.

Sulfinalol is a compound that acts as an orally active β-adrenoceptor antagonist and directly induces vasodilation [1].

RX821002 is a potent and selective antagonist of α2-adrenoceptor with low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

Fenoldopam hydrochloride is a selective D1-like dopamine receptor partial agonist. It acts as a vasodilator in vivo and does not readily cross the blood-brain barrier. Fenoldopam HCl is also an α2-adrenoceptor antagonist in vitro.

Cicloprolol (free base) is a beta-adrenoceptor antagonist.

L 654284 is a potent and selective alpha 2 adrenoceptor antagonist.

LK 204-545 is a highly selective antagonist of beta1-adrenoceptor.

GYKI-12743 HCl is a postsynaptic vascular alpha-adrenoceptor antagonist.

Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.