TY - JOUR AU - Chen Zhong-jian AU - Minneman Kenneth P PY - 2016 TI - Recent progress in alpha 1 -adrenergic receptor research JF - Acta Pharmacologica Sinica; Vol 26, No 11 (November 2005): Acta Pharmacologica Sinica Y2 - 2016 KW - N2 - alpha 1 -Adrenergic receptors (AR) play an important role in the regulation of physiological responses mediated by norepinephrine and epinephrine, particularly in the cardiovascular system. The three cloned alpha1-AR subtypes (alpha 1A , alpha 1B , and alpha 1D ) are G protein-coupled receptors that signal through the G q /11 signaling pathway, each showing distinct pharmacological properties and tissue distributions. However, due to the lack of highly subtype-selective drugs, the functional roles of individual subtypes are still not clear. Development of new subtype-specific drugs will greatly facilitate the identification of the functions of each subtype. Conopeptide p-TIA has been found to be a new alpha 1B -AR selective antagonist with different modes of inhibition at alpha 1 -AR subtypes. In addition, recent studies using genetically engineered mice have shed some light on alpha 1 -AR functions in vivo , especially in the cardiovascular system and brain. Several proteins have been shown to interact directly with particular alpha 1 -AR, and may be important in regulating receptor function. Receptor heterodimerization has been shown to be important for cell surface expression, signaling and internalization. These new observations are likely to help elucidate the functional roles of individual alpha 1 -AR subtypes. UR - http://www.chinaphar.com/article/view/3915