Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.
Khatuya
Haripada
H
Drug Discovery Research, Johnson & Johnson Pharmaceutical Research and Development LLC, Raritan, NJ 08869, USA.
Hutchings
Richard H
RH
Kuo
Gee-Hong
GH
Pulito
Virginia L
VL
Jolliffe
Linda K
LK
Li
Xiaobing
X
Murray
William V
WV
D018674:Adrenergic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D058668:Adrenergic alpha-1 Receptor Antagonists; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007555:Isoxazoles; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology; D011485:Protein Binding; D018340:Receptors, Adrenergic, alpha-1; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
C547713:ADRA1A protein, human; D018674:Adrenergic Antagonists; D058668:Adrenergic alpha-1 Receptor Antagonists; D006576:Heterocyclic Compounds, 4 or More Rings; D007555:Isoxazoles; D010879:Piperazines; D018340:Receptors, Adrenergic, alpha-1