Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia
| Autor: | Xianhai Huang, Anandan Palani, John Cook, Stan Kurowski, Constance Farley, Jun Qin, Madhu Chintala, Xiaohong Zhu, Margaret van Heek, Ying Huang, Hongtao Zhang, Boonlert Cheewatrakoolpong, Sylvia J. Degrado, Ashwin U. Rao, Scott Greenfeder, Fangbiao Li, Qiu Li, Dong Xiao, Xiao Chen, Ganfeng Wang, Yunsheng Hsieh, Zhidan Liu, Robert G. Aslanian |
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| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
Agonist
medicine.medical_specialty Very low-density lipoprotein Side effect medicine.drug_class Upper body business.industry Organic Chemistry Pharmacology medicine.disease Biochemistry Endocrinology Nicotinic agonist Internal medicine Drug Discovery medicine lipids (amino acids peptides and proteins) business Receptor Dyslipidemia Lipoprotein |
| Popis: | Nicotinic acid has been used clinically for decades to control serum lipoproteins. Nicotinic acid lowers very low-density lipoprotein (VLDL)-cholesterol, low-density lipoprotein (LDL)-cholesterol, and lipoprotein-a (LPa), and it is also effective in raising high-density lipoprotein (HDL)-cholesterol. However, nicotinic acid has several side effects in clinical use. The most notable is intense cutaneous vasodilation “flushing” on the upper body and face. We discovered a pyranopyrimidinedione series to be nicotinic acid receptor agonists. A potent nicotinic acid receptor agonist from this series {5-(3-cyclopropylpropyl)-2-(difluoromethyl)-3H-pyrano[2,3-d]pyrimidine-4,7-dione}with reduced flushing side effect in dogs was identified. |
| Databáze: | OpenAIRE |
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