title: The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.
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.
authors.affiliation: Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA.
authors.forename: X
authors.initials: X
authors.lastname: Tian
authors.forename: L W
authors.initials: LW
authors.lastname: Hsin
authors.forename: E L
authors.initials: EL
authors.lastname: Webster
authors.forename: C
authors.initials: C
authors.lastname: Contoreggi
authors.forename: G P
authors.initials: GP
authors.lastname: Chrousos
authors.forename: P W
authors.initials: PW
authors.lastname: Gold
authors.forename: K
authors.initials: K
authors.lastname: Habib
authors.forename: A
authors.initials: A
authors.lastname: Ayala
authors.forename: W C
authors.initials: WC
authors.lastname: Eckelman
authors.forename: A E
authors.initials: AE
authors.lastname: Jacobson
authors.forename: K C
authors.initials: KC
authors.lastname: Rice
mesh_terms: 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
chemical_list: 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