Clinical pharmacology of β3 -adrenoceptors

Can [125I]-Iodocyanopindolol Label β3-Adrenoceptors in Rat Urinary Bladder?

β(3)-Adrenoceptors have been demonstrated to mediate urinary bladder smooth muscle relaxation but proof of their expression at the protein level has been missing because of lack of suitable antibodies or radioligands. As among various available radioligands [(125)I]-iodocyanopindolol ([(125)I]-ICYP) exhibited the smallest problems in labeling cloned human β(3)-adrenoceptors in previous studies,...

β3-adrenoceptors inhibit stimulated norepinephrine release in spontaneously hypertensive rats

Here, the influence of β3-adrenoceptors on catecholamine release in normotensive and spontaneously hypertensive rats was analyzed. Blood pressure was recorded through a femoral artery catheter, and cardiac output by ascending aorta flow. Time from onset of flow to maximum rise in flow indicated inotropy. Total peripheral vascular resistance (TPR) was calculated. Norepinephrine release was stimu...

The odd sibling: features of β3-adrenoceptor pharmacology.

β3-Adrenoceptor agonists have recently been introduced for the treatment of overactive urinary bladder syndrome. Their target, the β3-adrenoceptor, was discovered much later than β1- and β2-adrenoceptors and exhibits unique properties which make extrapolation of findings from the other two subtypes difficult and the β3-adrenoceptor a less-understood subtype. This article discusses three aspects...

Iv. International Union of Pharmacology Nomenclature of Adrenoceptors

Phenotype pharmacology of lower urinary tract α(1)-adrenoceptors.

α(1)-Adrenoceptors are involved in numerous physiological functions, including micturition. However, the pharmacological profile of the α(1)-adrenoceptor subtypes remains controversial. Here, we review the literature regarding α(1)-adrenoceptors in the lower urinary tract from the standpoint of α(1L) phenotype pharmacology. Among three α(1)-adrenoceptor subtypes (α(1A), α(1B) and α(1D)), α(1a)-...