The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1
Journal
Bioorganic and Medicinal Chemistry Letters
Journal Volume
11
Journal Issue
3
Pages
331-333
Date Issued
2001
Author(s)
Tian X.
Webster E.L.
Contoreggi C.
Chrousos G.P.
Gold P.W.
Habib K.
Ayala A.
Eckelman W.C.
Jacobson A.E.
Rice K.C.
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.
Type
journal article