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 …
selectivity for the cloned human α1a receptor. Systematic modifications of 12 led to …
Silodosin: an update on efficacy, safety and clinical indications in urology
Introduction Silodosin determines smooth muscle relaxation in bladder and prostate tissues,
increases bladder blood flow in conditions of chronic bladder ischemia and regulates the …
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 …
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 …
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 …
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 …
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) …
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 …
[({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
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 …
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 …
antagonists. Systematic modification of the lipophilic 4, 4-diphenylpiperidinyl moiety of the …