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

X Tian; L W Hsin; E L Webster; C Contoreggi; G P Chrousos; P W Gold; K Habib; A Ayala; W C Eckelman; A E Jacobson; K C Rice

doi:10.1016/s0960-894x(00)00661-2

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

Bioorg Med Chem Lett. 2001 Feb 12;11(3):331-3. doi: 10.1016/s0960-894x(00)00661-2.

Authors

X Tian¹, L W Hsin, E L Webster, C Contoreggi, G P Chrousos, P W Gold, K Habib, A Ayala, W C Eckelman, A E Jacobson, K C Rice

Affiliation

¹ Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA.

PMID: 11212103
DOI: 10.1016/s0960-894x(00)00661-2

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-propylpyrimidine-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.

MeSH terms

Animals
Cyclopropanes* / chemical synthesis
Cyclopropanes* / metabolism
Humans
Iodine Radioisotopes
Ligands
Protein Binding
Pyrimidines* / chemical synthesis
Pyrimidines* / metabolism
Radiopharmaceuticals*
Receptors, Corticotropin-Releasing Hormone / metabolism*
Structure-Activity Relationship
Tomography, Emission-Computed, Single-Photon / methods*

Substances

5-chloro-N-cyclopropylmethyl-N-(2,6-dichloro-4-iodophenyl)-2-methyl-N-propylpyrimidine-4,6-diamine
Cyclopropanes
Iodine Radioisotopes
Ligands
Pyrimidines
Radiopharmaceuticals
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1