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

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

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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

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.

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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.",

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