The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.
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.
Tian
X
X
Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA.
Hsin
L W
LW
Webster
E L
EL
Contoreggi
C
C
Chrousos
G P
GP
Gold
P W
PW
Habib
K
K
Ayala
A
A
Eckelman
W C
WC
Jacobson
A E
AE
Rice
K C
KC
D000818:Animals; D003521:Cyclopropanes / Q000138:chemical synthesis / Q000378:metabolism; D006801:Humans; D007457:Iodine Radioisotopes; D008024:Ligands; D011485:Protein Binding; D011743:Pyrimidines / Q000138:chemical synthesis / Q000378:metabolism; D019275:Radiopharmaceuticals; D018019:Receptors, Corticotropin-Releasing Hormone / Q000378:metabolism*; D013329:Structure-Activity Relationship; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*; D000099052:CRF Receptor, Type 1
C427024:5-chloro-N-cyclopropylmethyl-N-(2,6-dichloro-4-iodophenyl)-2-methyl-N-propylpyrimidine-4,6-diamine; D003521:Cyclopropanes; D007457:Iodine Radioisotopes; D008024:Ligands; D011743:Pyrimidines; D019275:Radiopharmaceuticals; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1