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

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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-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.

A high affinity radioligand for CRHR1 has been prepared that can serve as a template for the development of SPECT imaging agents.

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Acknowledgements

The authors thank Noel Whittaker and Wesley White of the Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, for the mass spectral data.

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Current Address: Procter & Gamble Pharmaceuticals, HCRC, Mason, OH 45040, USA.

Current Address: University of Medicine and Dentistry of New Jersey, Robert Wood Johnson Medical School, Department of Pharmacology, Piscataway, NJ 08854, USA.

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Current Address: University of North Carolina, Department of Psychiatry, Chapel Hill, NC 27599, USA.

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