Design and Synthesis of Novel α1a Adrenoceptor-Selective Antagonists. 1. Structure−Activity Relationship in Dihydropyrimidinones

D Nagarathnam, SW Miao, B Lagu, G Chiu… - Journal of medicinal …, 1999 - ACS Publications
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype
selectivity for the cloned human α1a receptor. Systematic modifications of 12 led to …

Silodosin: an update on efficacy, safety and clinical indications in urology

L Villa, P Capogrosso, U Capitanio, A Martini… - Advances in …, 2019 - Springer
Introduction Silodosin determines smooth muscle relaxation in bladder and prostate tissues,
increases bladder blood flow in conditions of chronic bladder ischemia and regulates the …

KMD-3213, a uroselective and long-acting α1a-adrenoceptor antagonist, tested in a novel rat model

K Akiyama, M Hora, S Tatemichi, N Masuda… - … of Pharmacology and …, 1999 - ASPET
KMD-3213, an α1a-adrenoceptor (AR) antagonist, is under development for the treatment of
urinary outlet obstruction in patients with benign prostatic hypertrophy. In the present study …

Silodosin for the treatment of clinical benign prostatic hyperplasia: safety, efficacy, and patient acceptability

HJ Cho, TK Yoo - Research and Reports in Urology, 2014 - Taylor & Francis
α1-Adrenergic receptor antagonists are commonly used to treat male lower urinary tract
symptoms and benign prostatic hyperplasia (BPH). We performed a literature search using …

Tissue selectivity of KMD-3213, an α1-adrenoceptor antagonist, in human prostate and vasculature

S MURATA, T TANIGUCHI, M TAKAHASHI… - The Journal of …, 2000 - Elsevier
PURPOSE: We evaluated the binding and functional affinity of KMD-3213 and other α1-
adrenoceptor (AR) antagonists such as prazosin or tamsulosin, to compare the tissue …

Effects of tamsulosin and silodosin on isolated albino and pigmented rabbit iris dilators: possible mechanism of intraoperative floppy-iris syndrome

T Goseki, H Ishikawa, S Ogasawara, K Mashimo… - Journal of Cataract & …, 2012 - Elsevier
PURPOSE: To determine the mechanism of intraoperative floppy-iris syndrome (IFIS) by
examining the binding affinity of tamsulosin and silodosin to α-receptors and melanin …

Pharmacological analysis of the novel, selective α1‐adrenoceptor antagonist, KMD‐3213, and its suitability as a tritiated radioligand

S Murata, T Taniguchi… - British journal of …, 1999 - Wiley Online Library
Pharmacological profiles of tritiated KMD‐3213, a new antagonist of α1‐adrenoceptor (AR),
were examined in recombinant and native α1‐AR, and compared with those of prazosin (PZ) …

In vitro studies on L-771,688 (SNAP 6383), a new potent and selective α1A-adrenoceptor antagonist

RSL Chang, TB Chen, SS O'Malley… - European journal of …, 2000 - Elsevier
L-771,688 (SNAP 6383, methyl (4S)-4-(3, 4-difluorophenyl)-6-[(methyloxy) methyl]-2-oxo-3-
[({3-[4-(2-pyridinyl)-1-piperidinyl] propyl} amino) carbonyl]-1, 2, 3, 4-tetrahydro-5 …

Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective α1A-Adrenoceptor Antagonists

F Zhao, J Li, Y Chen, Y Tian, C Wu, Y Xie… - Journal of Medicinal …, 2016 - ACS Publications
A series of indoline and indole derivatives were designed, synthesized, and evaluated as
selective α1A-adrenergic receptor (α1A-AR) antagonists for the treatment of benign prostatic …

Design and Synthesis of Novel α1a Adrenoceptor-Selective Dihydropyridine Antagonists for the Treatment of Benign Prostatic Hyperplasia

D Nagarathnam, JM Wetzel, SW Miao… - Journal of medicinal …, 1998 - ACS Publications
We report the synthesis and evaluation of novel α1a adrenoceptor subtype-selective
antagonists. Systematic modification of the lipophilic 4, 4-diphenylpiperidinyl moiety of the …