Bodilisant鈥擜 Novel Fluorescent, Highly Affine Histamine H3 Receptor Ligand

详细信息    查看全文

• 作者：Miriam Tomasch ; J. Stephan Schwed ; Alexander Paulke ; Holger Stark
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：February 14, 2013
• 年：2013
• 卷：4
• 期：2
• 页码：269-273
• 全文大小：269K
• 年卷期：v.4,no.2(February 14, 2013)
• ISSN：1948-5875

文摘

A piperidine-based lead structure for the human histamine H₃ receptor (hH₃R) was coupled with the BODIPY fluorophore and resulted in a strong green fluorescent (quantum yield, 0.92) hH₃R ligand with affinity in the nanomolar concentration range (K_i hH₃R = 6.51 卤 3.31 nM), named Bodilisant. Screening for affinities at histamine and dopamine receptor subtypes showed high hH₃R preference. Bodilisant was used for visualization of hH₃R in hH₃R overexpressing HEK-293 cells with fluorescence confocal laser scanning microscopy. In addition, in native human brain tissues, Bodilisant showed clear and displaceable images of labeled hH₃R.

Keywords:

histamine; H₃ receptor; nonimidazole derivative; GPCR; BODIPY; HEK-293 cells; tissue labeling; fluorescence confocal laser scanning microscopy; displacement; pharmacological tool