Effect of a novel benzamide, YM-09151-2, on rat serum prolactin levels

Add time:08/21/2019    Source:sciencedirect.com

YM-09151-2(cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide) is a new benzamide which has been reported to be an antagonist of dopamine (DA) at D1-type DA receptors. In the present study, we have examined the extent of the interaction of YM-09151-2 with D2-type DA receptors in the anterior pituitary gland of the rat. YM-09151-2 was found to be a potent antagonist of these receptors as extremely low doses of this compound produced a marked, dose-dependent elevation of serum prolactin concentrations. This benzamide was also a potent blocker 3f DA-induced inhibition of prolactin release invitro and was very effective in displacing 3H-spiperone from bovine pituitary membranes: IC50, 1.04nM. These results are consistent with recent evidence that YM-09151-2 is also a potent antagonist of the D2-type receptors in the intermediate lobe of the rat pituitary gland.

We also recommend Trading Suppliers and Manufacturers of YM 435 (cas 138086-00-7). Pls Click Website Link as below: cas 138086-00-7 suppliers

Prev:Adrenoceptor blocking, hemodynamic and coronary effects of YM-09538, a new combined α- and β-adrenoceptor blocking drug, in anesthetized dogs
Next:The Discovery of YM-60828: A Potent, Selective and Orally-Bioavailable Factor Xa Inhibitor)