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 R Ayala, William C. Eckelman, Arthur E. Jacobson, Kenner C. Rice

Research output: Contribution to journalArticle

18 Citations (Scopus)

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

Fingerprint

Single photon emission computed tomography
Diamines
Single-Photon Emission-Computed Tomography
Imaging techniques
CRF receptor type 1

ASJC Scopus subject areas

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

Cite this

The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1. / Tian, Xinrong; Hsin, Ling Wei; Webster, Elizabeth L.; Contoreggi, Carlo; Chrousos, George P.; Gold, Philip W.; Habib, Kamal; Ayala, Alejandro R; Eckelman, William C.; Jacobson, Arthur E.; Rice, Kenner C.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 3, 12.02.2001, p. 331-333.

Research output: Contribution to journalArticle

Tian, Xinrong ; Hsin, Ling Wei ; Webster, Elizabeth L. ; Contoreggi, Carlo ; Chrousos, George P. ; Gold, Philip W. ; Habib, Kamal ; Ayala, Alejandro R ; Eckelman, William C. ; Jacobson, Arthur E. ; Rice, Kenner C. / The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 3. pp. 331-333.
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AU - Chrousos, George P.

AU - Gold, Philip W.

AU - Habib, Kamal

AU - Ayala, Alejandro R

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AU - Jacobson, Arthur E.

AU - Rice, Kenner C.

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