Publications by authors named "Eiji Kawaminami"
Article Synopsis
- The M muscarinic acetylcholine receptor (mAChR) is important for mediating acetylcholine's effects in both peripheral and central nervous systems, but understanding its functions has been limited by the lack of specific agonists and positive allosteric modulators (PAMs).
- Through a structured activity relationship (SAR) study of a thiazole derivative, researchers discovered new N-pyrimidyl/pyridyl-2-thiazolamine analogues that showed unique conformational characteristics essential for pharmacological activity through sulfur-nitrogen nonbonding interactions.
- Among these analogues, compound 3g demonstrated strong PAM activity with excellent subtype selectivity and positive pharmacological effects on
Current pharmacotherapies for lower urinary tract symptoms associated with benign prostate hyperplasia (LUTS/BPH) are in need of improvement. Lysophosphatidic acid (LPA) is a phospholipid with various biologic functions. However, its exact role in the lower urinary tract and its target receptor subtype have not been fully elucidated.
View Article and Find Full Text PDFA novel series of N-arylpiperazine-1-carboxamide derivatives was synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Reporter assays indicated that trans-2,5-dimethylpiperazine derivatives are potent AR antagonists, and in this series trans-N-4-[4-cyano-3-(trifluoromethyl)phenyl]-N-(2,4-difluorophenyl)-2,5-dimethylpiperazine-1-carboxamide (18 g, YM-175735) exhibited the most potent antiandrogenic activity. Compared to bicalutamide, YM-175735 is an approximately 4-fold stronger AR antagonist and has slightly increased antiandrogenic activity, suggesting that YM-175735 may be useful in the treatment of prostate cancer.
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