Abstract
A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood-brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Autoradiography
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Blood-Brain Barrier
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Brain / metabolism
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Bromine Radioisotopes
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In Vitro Techniques
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Ligands
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / metabolism
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Receptors, Corticotropin-Releasing Hormone / metabolism*
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Tissue Distribution
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Triazines / chemical synthesis*
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Triazines / metabolism
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Triazines / pharmacokinetics
Substances
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Bromine Radioisotopes
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Ligands
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MJL 1-109-2
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Radiopharmaceuticals
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Receptors, Corticotropin-Releasing Hormone
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Triazines
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CRF receptor type 1