α1d-adrenoceptor

α1A/1D-Adrenoceptor antagonist-1 is a dual-targeting adrenoceptor antagonist exhibiting exceedingly high binding affinity for both alpha 1A and alpha 1D subtypes. It significantly reduces urethral resistance by specifically blocking smooth muscle contraction in the lower urinary tract and prostate, serving as an important tool for investigating benign prostatic hyperplasia (BPH) and hypertension mechanisms.

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.

Rec 15/2615 dihydrochloride is an antagonist of α1B-adrenergic receptor.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Xylometazoline hydrochloride (Xylometazoline HCl) is an α-adrenoceptor agonist usually used as nasal decongestant.

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.

Silodosin (KAD 3213) is an alpha-Adrenergic Blocker. The mechanism of action of silodosin is as an Adrenergic alpha-Antagonist.

ADRA1D receptor antagonist 1 HCl is an orally active, potent and selective α1D adrenergic receptor antagonist (Ki: 1.6 nM) with potential antiproliferative activity.

(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).

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

(S)-Terazosin is an active S-enantiomer of Terazosin and acts as a potent, high-affinity antagonist of α-adrenoceptors [α1a, α1b, and α1d-adrenoceptors] with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively.

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

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

Desglymidodrine (ST 1059) is a selective α1-adrenoceptor agonist and an active metabolite of Midodrine. It is a vasoconstrictor that can be used for cardiovascular research and neurocardiogenic syncope.

RS 504393 is a highly selective CCR2 chemokine receptor antagonist (IC50s: 89 nM and > 100 μM for human recombinant CCR2 and CCR1).

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.

Fiduxosin hydrochloride is an alpha 1a-adrenoceptor antagonist that may be useful in the treatment of Benign Prostatic Hyperplasia.

SUN-1334H free base, an orally active histamine H1 receptor inhibitor, exhibits a K_i of 9.7 nM and an IC 50 of 20.3 nM. Additionally, it effectively prevents histamine-induced contractions in isolated guinea-pig ileum with an IC 50 of 0.198 μM. The compound also blocks histamine-induced bronchoconstriction and skin wheals in guinea pigs and beagle dogs, respectively, and mitigates ovalbumin-induced rhinitis in guinea pigs.

MT-1207 is a selective antagonist of adrenergic α1 and 5-HT2A receptors with oral activity. It exhibits IC50 values of <0.1 nM for α1A, 0.15 nM for α1B, 1.40 nM for α1D, and 0.27 nM for 5-HT2A. In the 2K2C rat model, MT-1207 effectively reduces blood pressure (BP) without impairing renal function. As a multitarget inhibitor, MT-1207 has potential for research in vasodilation.

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.

RS102895 is a potent CCR2 antagonist (IC50: 360 nM) and shows no effect on CCR1.

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).

PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.