10463-21-5Relevant academic research and scientific papers
N-phenyl>methanesulfonamide. A Potent Agonist Which Releases Intracellular Calcium by Activation of α1-Adrenoceptors
DeMarinis, Robert M.,Lavanchy, Patricia,Hieble, J, Paul,Jim, Kam F.,Matthews, William D.
, p. 245 - 248 (1985)
N-phenyl>methanesulfonamide (SKandF 102652) has been prepared and characterized pharmacologically.It is a potent agonist with an EC50 of 25 nM at α1-adrenoceptors as determined in the isolated perfused rabbit
Compounds and Compositions for Modulating Lipid Levels and Methods of Preparing Same
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Page/Page column 42, (2011/02/15)
The present technology relates to compounds of Formulas I-VI and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also increase HDL-C, lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.
CORYDALINE DERIVATIVES USEFUL FOR REDUCING LIPID LEVELS
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Page/Page column 120, (2010/07/09)
The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL- cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated potein kinase.
Synthesis and Evaluation of Non-Catechol D-1 and D-2 Dopamine Receptor Agonists: Benzimidazol-2-one, Benzoxazol-2-one, and the Highly Potent Benzothiazol-2-one 7-Ethylamines
Weinstock, Joseph,Gaitanopoulos, Dimitri E.,Stringer, Orum D.,Franz, Robert G.,Hieble, J. Paul,et al.
, p. 1166 - 1176 (2007/10/02)
Our interest in identifying D-1 and D-2 dopamine receptor agonists that are not catechols led us to extend previous studies with oxindoles by investigating analogues of dopamine, N,N-dipropyldopamine, m-tyramine, N,N-dipropyl-m-tyramine, and epinine in which the m-hydroxyl is replaced by the NH portion of a thiazol-2-one, oxazol-2-one, or imidazol-2-one group fused to the 2,3-position.These compounds were evaluated for their affinity and agonist activity at D-1 and D-2 receptors by using in vitro assays.Replacement of the m-hydroxy in N,N-dipropyldopamine with the thiazol-2-one group resulted in a dramatic increase in D-2 receptor affinity and activity compared to that of N,N-dipropyldopamine itself or that of the corresponding oxindole, 1.The resulting compound, 7-hydroxy-4-benzothiazol-2(3H)-one (4), is the most potent D-2 receptor agonist reported to date in the field-stimulated rabbit ear artery (ED50=0.028 nM).The benzoxazol-2-one (6), benzimidazol-2-one (5), and isatin (51) analogues showed D-2 receptor agonist potency similar to that of 1.The des-7-hydroxy analogues of 4 (21) also has enhanced D-2 receptor activity compared to that of the corresponding oxindole, 8. 7-Hydroxy-4-(2-aminoethyl)benzothiazol-2(3H)-one, 27, a non-catechol, has enhanced D-1 and D-2 receptor activity in vitro compared to that of the corresponding oxindole, 7.In vivo, 27 increased renal blood flow and decreased blood in the dog.However, these effects were mediated primarily by D-2 receptor agonist activity.This may be a result of the D-1 partial agonist activity of 27 coupled with its potent D-2 receptor activity.
