[125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor
摘要：
Shortened, more stable and weakly hydrophobic analogues of melanin-concentrating hormone (MCH) were searched as candidates for radioiodination. Starting from the dodecapeptide MCH<sub>6 – 17</sub>, we found that: (1) substitution of Tyr<sup>13</sup> by a Phe residue; (2) addition of a 3-iodo-Tyr residue at the N-terminus; and (3) addition of a hydrophilic spacer 8-amino-3,6-dioxyoctanoyl between the 3-iodo-Tyr and MCH<sub>6 – 17</sub> (compound S36057), led to an agonist more potent than MCH itself in stimulating [<sup>35</sup>S]-GTPγS binding at membranes from HEK293 cells stably expressing the human MCH receptor.
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关键词：
[<sup>125</sup>I]-(3-iodo Tyr<sup>13</sup>)-MCH binding [<sup>125</sup>I]-S36057 binding MCH SLC-1 receptor
DOI：
10.1038/sj.bjp.0704085
被引量：
年份：
2001
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