Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
摘要:
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.
Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
摘要:
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.
申请人:NATIONAL INSTITUTE OF INFORMATION AND COMMUNICATIONS
TECHNOLOGY
公开号:US20210032228A1
公开(公告)日:2021-02-04
The present invention provides an electro-optic polymer (EO polymer) comprising an electro-optic molecule (EO molecule) and a base polymer. The EO polymer of the present invention has good performance over the entire optical communication wavelength range and therefore can preferably be used for the production of optical modulators, optical switches, optical transceivers, optical phased arrays, LiDAR (light detection and ranging) devices, electric field sensors, terahertz wave generators and detectors, etc.
Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b
作者:Jae-Kyu Jung、Benjamin R. Johnson、Tracy Duong、Marc Decaire、Jane Uy、Tawfik Gharbaoui、P. Douglas Boatman、Carleton R. Sage、Ruoping Chen、Jeremy G. Richman、Daniel T. Connolly、Graeme Semple
DOI:10.1021/jm070022x
日期:2007.4.1
Recently identified GPCRs, GPR109a and GPR109b, the high and low affinity receptors for niacin, may represent good targets for the development of HDL elevating drugs for the treatment of atherosclerosis. Acifran, an agonist of both receptors, has been tested in human subjects, yet until recently very few analogs had been reported. We describe a series of acifran analogs prepared using newly developed synthetic pathways and evaluated as agonists for GPR109a and GPR109b, resulting in identification of compounds with improved activity at these receptors.