Enhancing the selectivity of alpha2-adrenoceptor (α2A-AR) agonists remains an unresolved
issue. Herein, we reported the design of an α2A-AR agonist using the conformation …

In this study four and five-feature pharmacophores for selective antagonists at each of the
three α1-adrenoceptor (AR) subtypes were used to identify novel α1-AR subtype selective …

α1A-, α1B-, and α1D-adrenoceptors (α1-ARs) are members of the adrenoceptor G protein-
coupled receptor family that are activated by adrenaline (epinephrine) and noradrenaline …

ABSTRACT α 1-Adrenergic receptor (AR) blockers can be effective for the treatment of
benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited …

Beginning from the screening hit and literature α1-adrenergic compounds, a hybridized
basic skeleton A was proposed as the pharmacophore for potent and selective α1a-AR …

A number of (S)-and (R)-2-[(2-phenoxyethyl) aminomethyl]-1, 4-benzodioxanes
unsubstituted or ortho monosubstituted at the phenoxy moiety were synthesized and tested …

Indole-arylpiperazine derivatives have exhibited good selectivity for the α1A-adrenoceptor,
but the structure-activity-binding mechanism relationship remains unclear. In the current …

Finding effective chemotherapeutic agents for clinical use is a long‐lasting goal in medicinal
chemistry. In this study, we report a new class of α1‐adrenoceptor (α1‐AR) antagonists …

Our previous structure− affinity relationship study had considered the enantiomers of the
naphthodioxane, tetrahydronaphthodioxane, and 2-methoxy-1-naphthoxy analogues …

Starting from two acridine compounds identified in a high-throughput screening campaign (1
and 2, Table 1), a series of 4-aminoquinolines was synthesized and tested for their …