α1-adrenoceptor

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

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.

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

Tolnapersine is a mixed dopamine agonist and alpha-adrenoceptor antagonist.

Saterinone is a potent and selective phosphodiesterase III inhibitor and a potent antagonist of the vascular α-1-adrenoceptor. Saterinone has vasodilatory properties and can be used in the acute treatment of chronic heart failure. Saterinone inhibited crude cAMP phosphodiesterase (PDE) activity in guinea pig right ventricular homogenates The ic50 value is 2.3 × 10(-5) mol/l.

Terazosin hydrochloride (Hytrin) , a selective alpha1-antagonist, can treat the benign prostatic hyperplasia (BPH). It also can lower blood pressure, so it is a drug of choice for patients with prostate enlargement and hypertension. It works on the smooth muscle of the bladder and the blood vessel walls by blocking the function of adrenaline.

DL-Norepinephrine hydrochloride (DL-lysine) is a high-affinity basic amino acid substrate of amino acid transporter b0 + with a Km value in the range of 100-400 μM.

Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.

AR-A 2 is a selective 5-HT1B receptor antagonist with high affinity to guinea pig cortex 5-HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM), exhibiting a 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

Pimozide-D4 is a deuterium labeled Pimozide (TMSM-3626).

(R)-Terazosin is an active R-enantiomer of Terazosin and 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).

Midodrine ((±)-Midodrin), an adrenergic alpha-1 agonist, belongs to the class of medications known as vasopressors.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

Terazosin hydrochloride dihydrate (Heitrin dihydrate) is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).

Ajmalicine (Raubasine) (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity.

Naftopidil hydrochloride (BM-15275 hydrochloride) is a selective alpha1-adrenoceptor antagonist with Ki of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, respectively. Naftopidil hydrochloride has antiproliferative effects.

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.

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

α1 adrenoceptor-MO-1 (S enantiomer) has affinity at alpha 1 adrenergic receptor with alphalytic activity and analgesic action. It has more active than R enantiomer.

Clopimozide (R-29764) acts as a calcium channel antagonist and inhibits [3H] nilandipine binding.Clopimozide is a novel and orally available long-acting antischizophrenic psychostatic compound.

LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

Delequamine (RS 15385-197) is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

CGP 20712 A (CGP 20712 mesylate) is a selective and potent β1-adrenergic receptor antagonist (IC50: 0.7 nM) with antihypertensive activity, capable of reversing RKT-induced gastric relaxation.

(±)-Prenalterol (H 80/62) is a new cardioselective positive inotropic compound that is an agonist of beta-2- and beta-1-adrenergic receptors and can be used to study chronic congestive heart failure.