α1a-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.

L-771688 (SNAP 6383) is a novel potent and selective α1A-adrenoceptor antagonist with a Ki value of 0.43±0.02 nM.L-771688 KE is used for the treatment of benign prostatic hyperplasia.

RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays.

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.

Nicergoline (Nicergolinum) is an ergot derivative used to treat senile dementia and other disorders with vascular origins.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

(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.

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

(R)-(-)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker and α1A-adrenoceptor antagonist.

α1A-adrenoceptor antagonist

L-771688 is an α1A-adrenoceptor antagonist potentially for the treatment of benign prostatic hyperplasia.

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.

Garomefrine HCl, a α1A-adrenoceptor agonist, is potential for the treatment of urinary incontinence.

Ro-70-0004 is a selective antagonist of alpha1A-adrenoceptor.

RS 100329 HCl is a selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors).

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

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).

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