The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1

Xinrong Tian, Ling Wei Hsin, Elizabeth L. Webster, Carlo Contoreggi, George P. Chrousos, Philip W. Gold, Kamal Habib, Alejandro Ayala, William C. Eckelman, Arthur E. Jacobson, Kenner C. Rice

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

A high-affinity radioligand for CRHR1 has been prepared that can serve as a template for the development of SPECT imaging agents. The 5-chloro-N-cyclopropylmethyl-N-(2,6-dichloro-4-iodophenyl)-2-methyl-N-propylp yrimidine-4,6-diamine (6b, Ki = 14 nM), and the corresponding 4-bromophenyl analogue (6a, Ki = 21 nM), were synthesized in four steps from compound 3.

Original languageEnglish (US)
Pages (from-to)331-333
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number3
DOIs
StatePublished - Feb 12 2001
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Tian, X., Hsin, L. W., Webster, E. L., Contoreggi, C., Chrousos, G. P., Gold, P. W., Habib, K., Ayala, A., Eckelman, W. C., Jacobson, A. E., & Rice, K. C. (2001). The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1. Bioorganic and Medicinal Chemistry Letters, 11(3), 331-333. https://doi.org/10.1016/S0960-894X(00)00661-2