The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1

Xinrong Tian; Ling Wei Hsin; Elizabeth L. Webster; Carlo Contoreggi; George P. Chrousos; Philip W. Gold; Kamal Habib; Alejandro Ayala; William C. Eckelman; Arthur E. Jacobson; Kenner 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 1

Xinrong Tian, Ling Wei Hsin, Elizabeth L. Webster, Carlo Contoreggi, George P. Chrousos, Philip W. Gold, Kamal Habib, Alejandro Ayala, William C. Eckelman, Arthur E. Jacobson, Kenner C. Rice

Research output: Contribution to journal › Article › peer-review

18 Scopus citations

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, K_i = 14 nM), and the corresponding 4-bromophenyl analogue (6a, K_i = 21 nM), were synthesized in four steps from compound 3.

Original language	English (US)
Pages (from-to)	331-333
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	3
DOIs	https://doi.org/10.1016/S0960-894X(00)00661-2
State	Published - Feb 12 2001
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/S0960-894X(00)00661-2

Fingerprint Dive into the research topics of 'The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1'. Together they form a unique fingerprint.

Cite this

Tian, X., Hsin, L. W., Webster, E. L., Contoreggi, C., Chrousos, G. P., Gold, P. W., Habib, K., Ayala, A., Eckelman, W. C., Jacobson, A. E., & Rice, K. C. (2001). The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1. Bioorganic and Medicinal Chemistry Letters, 11(3), 331-333. https://doi.org/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 1. / Tian, Xinrong; Hsin, Ling Wei; Webster, Elizabeth L.; Contoreggi, Carlo; Chrousos, George P.; Gold, Philip W.; Habib, Kamal; Ayala, Alejandro; 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 › peer-review

Tian, X, Hsin, LW, Webster, EL, Contoreggi, C, Chrousos, GP, Gold, PW, Habib, K, Ayala, A, Eckelman, WC, Jacobson, AE & Rice, KC 2001, 'The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1', Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 3, pp. 331-333. https://doi.org/10.1016/S0960-894X(00)00661-2

Tian, Xinrong ; Hsin, Ling Wei ; Webster, Elizabeth L. ; Contoreggi, Carlo ; Chrousos, George P. ; Gold, Philip W. ; Habib, Kamal ; Ayala, Alejandro ; Eckelman, William C. ; Jacobson, Arthur E. ; Rice, Kenner C. / The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 3. pp. 331-333.

@article{647b4c4102674b3f8532985f4643a768,

title = "The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1",

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.",

author = "Xinrong Tian and Hsin, {Ling Wei} and Webster, {Elizabeth L.} and Carlo Contoreggi and Chrousos, {George P.} and Gold, {Philip W.} and Kamal Habib and Alejandro Ayala and Eckelman, {William C.} and Jacobson, {Arthur E.} and Rice, {Kenner C.}",

year = "2001",

month = feb,

day = "12",

doi = "10.1016/S0960-894X(00)00661-2",

language = "English (US)",

volume = "11",

pages = "331--333",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "3",

}

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

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 -