α1-adrenoceptor

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.

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting 5-HT2 receptor antagonist (IC50: 0.9 nM), with less activity on Histamine H1, Dopamine D2, Adrenergic α1, and Adrenergic α2 receptors.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Dexmedetomidine hydrochloride (Precedex) is an imidazole derivative that is an agonist of the adrenergic alpha-2 receptor. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.

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.

Phenylephrine ((R)-(-)-Phenylephrine) is a selective α1-adrenoceptor agonist ( pKi: 5.86, 4.87 and 4.70 for α1D, α1B, and α1A receptors respectively).

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

Isoferulic acid (Hesperetate) exhibits hypoglycemic properties.

Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

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.

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.

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.

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.

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

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator that inhibits α1-adrenoceptor-mediated positive inotropic effects in a concentration-dependent manner, induced by contraction of isolated rabbit vascular smooth muscle.

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.

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.

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.

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.

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

(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).

NGB 2904 is a potent and selective antagonist of dopamine D3 receptor (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes mitogenesis stimulated by quinpirole (IC50 = 6.8 nM).

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

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).

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1 2 and Fyn kinase.

Alfuzosin (SL 77499) is an orally available, competitive α1-adrenoceptor antagonist.Alfuzosin induces smooth muscle relaxation in the bladder neck and prostate.Alfuzosin has been used to study benign prostatic hypertrophy, lower urinary tract symptoms (LUTS), and ejaculatory dysfunction (EjD).

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.

Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997).

HEAT hydrochloride is an α1-adrenoceptor antagonist.

D2343 is an agonist of β2-adrenoceptor. It also is an inhibitor of α1- adrenoceptor.

Doxazosin (UK 33274) is a long-acting α1-adrenoceptor inhibitor widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms.

Bunazosin is a potent and selective α1-adrenoceptor antagonist utilized in antihypertensive and ocular hypotensive research [1].

Terazosin-d8 is a deuterated compound of Terazosin. Terazosin has a CAS number of 63590-64-7. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment [1] [2] [3].

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

Medetomidine (Domtor) is a potent, highly selective α2-adrenoceptor agonist, demonstrating Ki values of 1.08 nM for α2-adrenoceptors and 1750 nM for α1-adrenoceptors, indicating significant selectivity for α2 over α1 receptors compared to clonidine and UK 14,304 with 1620-, 220-, and 300-fold respectively. Medetomidine significantly inhibits the twitch response in electrically stimulated mouse vas deferens (pD2 = 9.0), showcasing its efficacy. Exhibiting a wide range of pharmacological effects, Medetomidine is effective in vivo, manifesting hypotensive, bradycardic, sedative, anxiolytic, hypothermic, and analgesic properties.

Prazobind is a prazosinoid substance that blocks insulin stimulation of IP1 (inositol phosphate) accumulation and is an effective α1 adrenoceptor blocker.

(R)-(-)-Phenylephrine-2,4,6-d3 is a deuterated compound of (R)-(-)-Phenylephrine. (R)-(-)-Phenylephrine has a CAS number of 59-42-7. Phenylephrine is a selective α1-adrenoceptor agonist ( pKi: 5.86, 4.87 and 4.70 for α1D, α1B, and α1A receptors respectively).

Remoxipride hydrochloride (Roxiam) is a selective antagonist of D2 receptor with IC50s of 1.57 μM, ＞100 μM and 42 μM for D2 receptor, D1 receptor and α1-adrenoceptor.

Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.

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.

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.

Azepexole is a selective α2-adrenoceptor agonist that exhibits greater than 300-fold selectivity for the α2-adrenoceptor over the α1-adrenoceptor.

DL-Norepinephrine-d6 HCl is a deuterated compound of DL-NorepinephrineHCl. DL-NorepinephrineHCl has a CAS number of 55-27-6. DL-Norepinephrine hydrochloride is a high-affinity basic amino acid substrate of amino acid transporter b0 + with a Km value in the range of 100-400 μM.

NRA-0160 is a selective antagonist of dopamine D4 receptor(Ki of 0.48 nM)

Ajmalicine (Raubasine) hydrochloride, a potent adrenolytic compound, selectively inhibits α1-adrenoceptors and acts as a reversible, non-competitive full inhibitor of nicotine receptors with an IC50 of 72.3 μM. This chemical also serves as an anti-hypertensive and exhibits sedative activity, making it useful in various therapeutic applications.

2-PMDQ is an α1-adrenoceptor antagonist.