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Catalog No.
Product Name
Application
Product Information
Product Citation
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150
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5-HT1A and α1-adrenergic receptor antagonist
Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
α1-adrenoceptor antagonist
Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). -
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
alpha-1A/alpha-1B-adrenoceptor antagonist
Tamsulosin is an alpha1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH). -
β2 adrenergic antagonist
ICI 118551 hydrochloride is a selective β2 adrenergic antagonist. -
Adrenoceptors antagonist
BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration. -
Adrenergic α1 Receptor Antagonist
HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes. -
5-HT1A receptor antagonist
NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. -
α2-adrenergic receptor antagonist
Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM). -
Adrenoceptors antagonist
S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker. -
Adrenoceptors antagonist
(S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR. -
Adrenoceptors antagonist
SR 59230A hydrochloride is a β3-adrenoceptor antagonist. -
adrenergic receptor antagonist
Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro. -
α2 adrenergic receptor antagonist
Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant. -
alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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α1 receptor antagonist
Tamsulosin hydrochloride is a selective α1 receptor antagonist and a medicine which is used in benign prostatic hyperplasia. -
β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
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β-adrenergic receptors antagonist
Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. -
α1A antagonist
RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8). -
beta-adrenergic receptor antagonist
Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist. -
β-adrenergic receptor antagonist
(R)-Atenolol is a beta blocker used to treat high blood pressure and chest pain (angina). It can also reduce the risk of death after a heart attack. -
Non-selective β antagonist
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). -
α1A-adrenoceptor antagonist
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has been found to increase mental agility and enhance clarity and perception. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Nicergoline is used for vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs, Raynaud's disease, vascular migraines, and retinopathy. -
adrenoceptor antagonist
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity?=?255:1, a half-life of 4?min)?? acts as an adrenoceptor antagonist. -
β-adrenergic receptor antagonist
Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma. -
β-adrenergic receptor antagonist
Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity. -
α2 adrenoceptor antagonist
Piperoxan hydrochloride is an α2 adrenoceptor antagonist. -
peripheral adrenoceptor antagonist
Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors. -
β adrenergic receptor antagonist
Pargolol hydrochloride is a β adrenergic receptor antagonist. -
β adrenergic receptor antagonist
Spirendolol is a β adrenergic receptor antagonist. -
5-HT2A/α1-adrenergic receptor antagonist
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. -
ostsynaptic alpha adrenergic receptor antagonist
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist. -
α2-adrenoceptor antagonist
Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM. -
muscarinic receptor antagonist and β2-adrenoceptor agonist
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. -
β-adrenoceptor antagonist
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. -
β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
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beta-adrenoceptor antagonist
DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. .
