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 language | English |
|---|---|
| Pages (from-to) | 331-333 |
| Number of pages | 3 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 11 |
| Issue number | 3 |
| DOIs | |
| State | Published - Feb 12 2001 |
| Externally published | Yes |
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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 journal › Article
}
TY - JOUR
T1 - The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1
AU - Tian, Xinrong
AU - Hsin, Ling Wei
AU - Webster, Elizabeth L.
AU - Contoreggi, Carlo
AU - Chrousos, George P.
AU - Gold, Philip W.
AU - Habib, Kamal
AU - Ayala, Alejandro R
AU - Eckelman, William C.
AU - Jacobson, Arthur E.
AU - Rice, Kenner C.
PY - 2001/2/12
Y1 - 2001/2/12
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0035847696&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0035847696&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(00)00661-2
DO - 10.1016/S0960-894X(00)00661-2
M3 - Article
C2 - 11212103
AN - SCOPUS:0035847696
VL - 11
SP - 331
EP - 333
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 3
ER -