Adrenergics - Antagonists

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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.
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..
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
human ... ADRB1(153)
rat ... Adrb1(24925)
A143 (S)-(−)-Atenolol powder β1-Adrenergic receptor antagonist; active enantiomer of atenolol.
human ... ADRB1(153)
B016 Benoxathian hydrochloride solid Selective α1-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
B5683 Betaxolol hydrochloride >98% (HPLC) Selective β1 adrenoceptor antagonist.
human ... ADRB1(153)
B2185 Bisoprolol hemifumarate salt ≥98% (HPLC), solid Cardioselective β1-adrenoceptor antagonist.
B134 BMY 7378 dihydrochloride ≥98% (HPLC), solid BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.
human ... ADRA1D(146), HTR1A(3350)
B4559 BRL 44408 maleate salt ≥98% (HPLC) BRL 44408 maleate is a selective α2A-adrenoceptor antagonist.
C231 CGP-20712A methanesulfonate salt solid, ≥98% (HPLC) CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.
human ... ADRB1(153)
C247 Cyclazosin hydrochloride solid α1B-adrenoceptor antagonist.
D9815 Doxazosin mesylate ≥97% (HPLC), powder α1-adrenoceptor antagonist; relaxes smooth muscles of the prostate
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
rat ... Adra1a(29412), Adra1b(24173), Adra1d(29413)
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.
human ... ADRB2(154)
I2909 Indoramin hydrochloride ≥98% (HPLC), solid α1-adrenoceptor antagonist.
L1011 Labetalol hydrochloride >98% (TLC), powder Competitive β-adrenoceptor antagonist.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
U101 5-Methylurapidil solid Selective α1A-adrenoceptor antagonist; antihypertensive.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
M5391 (±)-Metoprolol (+)-tartrate salt ≥98% (titration), powder β1-adrenoceptor antagonist.
human ... ADRB1(153)
M5154 Moxisylyte hydrochloride >99% (TLC), powder α1-adrenoceptor antagonist; peripheral vasodilator.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
N158 Naftopidil hydrochloride hydrate solid α1-Adrenoceptor antagonist; antihypertensive.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
B019 Phenoxybenzamine hydrochloride ≥97%, powder Calmodulin antagonist; α-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
P7547 Phentolamine hydrochloride ≥98% (TLC), powder α-adrenoceptor antagonist; peripheral vasodilator.
P7561 Phentolamine methanesulfonate salt ≥98% (TLC), powder α-Adrenergic receptor antagonist; peripheral vasodilator.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
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.
human ... ADRB1(153), HTR1A(3350)
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
human ... ADRB1(153), HTR1A(3350), HTR1B(3351)
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.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P0689 (R)-(+)-Propranolol hydrochloride ≥98% (TLC) Less active enantiomer of propranolol.
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
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355)
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.
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358)
R9525 RX 821002 hydrochloride solid, ≥98% (HPLC) Selective α2-adrenoceptor antagonist
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
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.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
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
human ... ADRB3(155)
T4680 Terazosin hydrochloride ≥98% (TLC), powder α1-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
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.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
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.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), HTR1A(3350)
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.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)