Literature DB >> 11078336

Syntheses of the first endothelin-A- and -B-selective radioligands for positron emission tomography.

P Johnström1, F I Aigbirhio, J C Clark, S P Downey, J D Pickard, A P Davenport.   

Abstract

We have synthesized two potential positron emission tomography (PET) radioligands for the endothelin (ET) receptor. [11C]-PD156707 was produced by O-methylation of PD169390 using [11C]iodomethane. Radiochemical conversions of the order of 74 +/- 3.2% (n = 8) were obtained. The radiochemical purity of the isolated [11C]-PD156707 was 99% and the specific activity was 538 mCi/micromol. [18F]-BQ3020 was produced from [18F]fluoride in a total radiochemical yield of 2.7 +/- 0.4% (n = 10) in 238 +/- 5 min. The radiochemical purity was 95% and specific activities of the order of 670-930 mCi/micromol were obtained.

Entities:  

Mesh：

Substances：

Year:  2000        PMID： 11078336     DOI： 10.1097/00005344-200036001-00020

Source DB:  PubMed          Journal:  J Cardiovasc Pharmacol        ISSN： 0160-2446            Impact factor:   3.105


  3 in total

Review 1.  Positron emission tomography (PET): expanding the horizons of oncology drug development.

Authors:  Lisa A Hammond; Louis Denis; Umber Salman; Paul Jerabek; Charles R Thomas; John G Kuhn
Journal:  Invest New Drugs       Date:  2003-08       Impact factor: 3.850

2.  Positron emission tomography using 18F-labelled endothelin-1 reveals prevention of binding to cardiac receptors owing to tissue-specific clearance by ET B receptors in vivo.

Authors:  Peter Johnström; Tim D Fryer; Hugh K Richards; Neil G Harris; Olivier Barret; John C Clark; John D Pickard; Anthony P Davenport
Journal:  Br J Pharmacol       Date:  2005-01       Impact factor: 8.739

Review 3.  Endothelin.

Authors:  Anthony P Davenport; Kelly A Hyndman; Neeraj Dhaun; Christopher Southan; Donald E Kohan; Jennifer S Pollock; David M Pollock; David J Webb; Janet J Maguire
Journal:  Pharmacol Rev       Date:  2016-04       Impact factor: 25.468
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.