Antagonists- Adrenergics

Browse Sigma-Aldrich's list of antagonists specific for each of the adrenoceptor subtypes : α1, α2, β1, β2, and β3.

Adrenergic antagonists are drug molecule that blocks the function of adrenoceptor by receptor antagonism. Such antagonists cause cardiovascular effects including vasodilation. All β-adrenergic antagonists are competitive antagonists, while only some of the α-adrenergic antagonists are competitive.

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537075 (±)-Propranolol, Hydrochloride - CAS 3506-09-0 - Calbiochem A highly lipophilic agent that blocks both β₁ and β₂ adrenergic receptors with equal potency. A non-essential amino acid. Precursor of hydroxyproline in collagen. Cell permeable: no
Primary Target
β1 and β2 adrenergic receptors
Product does not compete with ATP.
Reversible: no
Target Ki: 17 nM for 5HT-1B receptors
M5391 (±)-Metoprolol (+)-tartrate salt ≥98% (titration), powder β1-adrenoceptor antagonist.
P0884 (±)-Propranolol hydrochloride ≥99% (TLC), powder Propranolol hydrochloride is a β-adrenoceptor antagonist. Its action at β2 receptor results in bronchoconstriction. Due to its lipophilic nature, propranolol can penetrate to the central nervous system and has a negative effect. It serves as a 5-HT1/5-HT2 serotonin receptor antagonist. Propranolol hydrochloride is useful as an antihypertensive drug, cardiac depressant and also in the treatment of angina pectoris. It decreases the effect of stress and exercise on heart by reducing the rate of contraction and conduction of impulse. It is known to competitively block the action of catecholamines.
S0278 (±)-Sotalol hydrochloride ≥98% (TLC), powder Potent β-adrenoceptor antagonist; class III antiarrhythmic; prolongs the action potential and increases the refractory period.
Sotalol has a potential to block non-cardioselective β-adrenergic receptors. It acts as an anti-arrhythmic agent and is used as a therapeutic for equine arrhythmias. In addition, sotalol also has an ability to stop atrial fibrillation recurrence.
5.05416 (+/-)-Atenolol - CAS 29122-68-7 - Calbiochem Primary Target
β₁ adrenergic receptor
P0689 (R)-(+)-Propranolol hydrochloride ≥98% (TLC) Less active enantiomer of propranolol.
A143 (S)-(−)-Atenolol powder β1-Adrenergic receptor antagonist; active enantiomer of atenolol.
P8688 (S)-(−)-Propranolol hydrochloride ≥98% (TLC), powder (S)-(−)-Propranolol hydrochloride is biologically active enantiomer. It acts as β1 receptor antagonist in thalamocortical neurons. (S)-(−)-Propranolol hydrochloride elicits its inhibitory function on the β1 adrenoceptor in trigeminovascular pain pathway and serves as a preventive medicine in migraine.
Active β-adrenoceptor blocking enantiomer, as measured by inhibition of isoprenaline-induced tachycardia; Propranolol is also non-specific 5-HT1A, 5-HT1B and 5-HT1C serotonin receptor antagonist. The stereoselective association of mianserin and propranolol with the 5HT1A, 5HT1B and 5HT1C sites may prove useful in the characterization of these sites
U101 5-Methylurapidil solid Selective α1A-adrenoceptor antagonist; antihypertensive.
A5736 ARC 239 dihydrochloride hydrate ≥98% (HPLC) ARC 239 is a selective α-2B adrenergic blocker. Although ARC-239, like prazosin, also has some alpha-1 antagonist activity, it is used most commomly to differentiate alpha-2A/D from alpha-2B and alpha-2C subtypes rather than for any alpha-1 inhibition..
A0232 Alfuzosin hydrochloride ≥98% (HPLC), solid Alfuzosin hydrochloride is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
B134 BMY 7378 dihydrochloride ≥98% (HPLC), solid BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.
B4559 BRL 44408 maleate salt ≥98% (HPLC) BRL 44408 maleate is a selective α2A-adrenoceptor antagonist.
B016 Benoxathian hydrochloride solid Selective α1-adrenoceptor antagonist.
B5683 Betaxolol hydrochloride >98% (HPLC) Selective β1 adrenoceptor antagonist.
B2185 Bisoprolol hemifumarate salt ≥98% (HPLC), solid Cardioselective β1-adrenoceptor antagonist.
C231 CGP-20712A methanesulfonate salt solid, ≥98% (HPLC) CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.
B003 Chloroethylclonidine dihydrochloride solid Irreversible α1B-adrenoceptor alkylating agent.
C247 Cyclazosin hydrochloride solid α1B-adrenoceptor antagonist.
SML1610 Dapiprazole hydrochloride ≥98% (HPLC) Dapiprazole hydrochloride is an an α-adrenergic blocking agent that is used to reverse mydriasis after eye examination.
D9815 Doxazosin mesylate ≥97% (HPLC), powder α1-adrenoceptor antagonist; relaxes smooth muscles of the prostate
SML0380 FMP-API-1 ≥98% (HPLC) FMP-API-1 is an inhibitor of AKAP-PKA interactions in vitro and in cultured cardiac myocytes that activates PKA. Apparently, FMP-API-1 binds to a novel allosteric regulatory site.
I127 ICI 118,551 hydrochloride ≥98% (HPLC), powder ICI 118,551 has been used to treat vasomotor migraines and somatic troubles related to anxiety state.
ICI 118,551 hydrochloride is a highly selective β2-adrenoceptor antagonist.
5.04746 Idazoxan Hydrochloride - CAS 79944-56-2 - Calbiochem Primary Target
→₂-adrenoceptor
I2909 Indoramin hydrochloride ≥98% (HPLC), solid α1-adrenoceptor antagonist.
5370   L-Proline - CAS 147-85-3 - Calbiochem  
L1011 Labetalol hydrochloride >98% (TLC), powder Competitive β-adrenoceptor antagonist.
SML1785 Landiolol hydrochloride ≥98% (HPLC) Landiolol is an ultra-short acting cardioselective β-adrenoceptor antagonist the exhibit β1-selectivity. New data shows that landiolol lacks pharmacochaperoning activity.
M7065 MK-912 hydrochloride hydrate ≥98% (HPLC) Selective α2-adrenoceptor antagonist
M5154 Moxisylyte hydrochloride >99% (TLC), powder α1-adrenoceptor antagonist; peripheral vasodilator.
N158 Naftopidil hydrochloride hydrate solid α1-Adrenoceptor antagonist; antihypertensive.
B019 Phenoxybenzamine hydrochloride ≥97%, powder Calmodulin antagonist; α-adrenoceptor antagonist.
P7547 Phentolamine hydrochloride ≥98% (TLC), powder α-adrenoceptor antagonist; peripheral vasodilator.
P7561 Phentolamine methanesulfonate salt ≥98% (TLC), powder α-Adrenergic receptor antagonist; peripheral vasodilator.
P0778 Pindolol ≥98% (TLC), powder β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator.
β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Pindolol is a non-cardioselective beta-adrenergic blocking agent. It possesses intrinsic sympathomimetic activity.
SML1462 Practolol ≥95% (HPLC) Practolol is a potent and selective β-adrenoceptor antagonist. Practolol is a beta blocker that was discontinued to due to adverse reactions (keratoconjunctivitis sicca, conjunctival scarring, fibrosis, metaplasia, and shrinkage).
P7791 Prazosin hydrochloride ≥99.0% (HPLC) Peripheral α1-adrenoceptor antagonist; vasodilator. Prazosin can be used to treat chronic posttraumatic stress disorder (PTSD). It plays a role in reducing blood pressure by relaxing blood vessels, hence used in the treatment of high blood pressure.
R9525 RX 821002 hydrochloride solid, ≥98% (HPLC) Selective α2-adrenoceptor antagonist
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
SML0581   SR 58894A ≥98% (HPLC) SR 58894A is also known as (3-(2-allylphenoxy)-1-[(1 S)-1,2,3,4-tetrahydronaphth-1-ylamino]-(2 S)-2-propanol hydrochloride, Kissei). It has the ability to antagonize relaxation, stimulated by isoprenaline.
SR58894A is a potent and selective antagonist of β3-adrenergic receptor.
S8688 SR 59230A ≥98% (HPLC), powder SR 59230A is a β3-adrenoceptor antagonist. It has high affinity for the β3 adrenoceptors occurring in human gut that affect the function of human colonic circular smooth muscle.1 It is reported that SR 59230A inhibits the Kir2.1-2.3 cardiac potassium channels.2
PZ0279   Sunepitron hydrochloride Sunepitron hydrochloride is a combined serotonin 5-HT1A receptor agonist and α2-adrenergic receptor antagonist. Sunepitron hydrochloride has been tested for the treatment of depression and anxiety.
T1330 Tamsulosin hydrochloride ≥98% (HPLC) Tamsulosin is an α1A/1D-adrenoceptor antagonist used as a treatment of benign prostatic hypertrophy (BPH). Its activity as an ? blocker also affects the iris, and has led to complications during cataract surgery, a condition called "floppy iris" syndrome.
T4680 Terazosin hydrochloride ≥98% (TLC), powder α1-adrenoceptor antagonist.
T6394 Timolol maleate salt ≥98% (TLC), powder Timolol maleate is a class II anti-arrhythmic agent that functions as a non-selective β-adrenoceptor antagonist, a vasodilator and an anti-glaucoma agent. Studies have reported that timolol maleate can be used for the treatment of infantile hemangioma (IH)7.
U100 Urapidil hydrochloride solid α1-adrenoceptor antagonist; 5-HT1A serotonin receptor partial agonist; anti-hypertensive.
The adrenoreceptor α 1a gene (ADRA1A) participates in smooth muscle contraction. It is also required for vasoconstriction of blood vessels throughout the body such as the skin, gastrointestinal system, genitourinary system, kidney and brain. ADRA1A plays a major role in glycogenolysis and gluconeogenesis of adipose tissue in the liver. It also plays a crucial role in sympathetic nervous system.
Y3125 Yohimbine hydrochloride ≥98% (HPLC), powder Yohimbine is derived from the Coryanthe yohimbe tree cortex. It is an alkaloid. Yohimbine hydrochloride is an α2-adrenergic receptor antagonist. It blocks the central α2-adrenergic receptors in the brain, thus preventing and reducing the effects of xylazine, an α2-adrenergic agonist. The sedative effects and respiratory depression that accompany xylazine administration are both antagonized and reversed by yohimbine. Yohimbine hydrochloride also produces an antidiuretic effect, and increases heart rate and blood pressure. It is useful in treating erectile dysfunction and promotes sexual functioning.