This review is intended to discuss recent developments in the molecula
r pharmacology of the alpha(1)-adrenergic receptor (alpha(1)-AR) subty
pes. After a brief historical development, we will focus on the more c
ontemporary issues having to do with this receptor family. Emphasis wi
ll be put on recent data regarding the cloning, nomenclature, signalli
ng mechanisms, and genomic organization of the alpha(1)-AR subtypes. W
e will also highlight recent mutational studies that identify key amin
o acid residues involved in ligand binding, as well as the role of the
alpha(1)-AR subtypes in regulating physiologic processes.