α1d-adrenergic receptor

Tamsulosin hydrochloride (Flomax hydrochloride) is the hydrochloride salt of tamsulosin, a sulfonamide derivative with α1 adrenergic antagonist activity.

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

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

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

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.

Phenylephrine hydrochloride (NCI-c55641) is a selective agonist of the α1-adrenergic receptor.

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.

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.

Cirazoline hydrochloride is a competitive full agonist of the α1A-adrenergic receptor (α1A-AR; Ki: 120 nM). It is a partial agonist at α1B-AR (Ki: 960 nM) and α1D-AR (Ki: 660 nM).

Conopeptide rho-TIA, a peptide from Conus tulipa venom, acts as a selective, noncompetitive inhibitor at the human α1B-Adrenergic Receptor and as a competitive inhibitor at the α1A and α1D-Adrenergic Receptors. Binding to these subtypes, conopeptide rho-TIA may inform the creation of new α1-Adrenergic Receptor subtype-selective drugs [1].

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

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).

(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).

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.

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.

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.

(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.

TAK-259 is a novel, selective, and orally active α1D adrenergic receptor antagonist (α1D, Ki = 1.1 nM) that represents a promising new therapeutic agent for the treatment of symptoms of OAB. It has an anti-frequency effect and reduces the burden of the hu

Cirazoline (free base) is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α₂ adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.

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.

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

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

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