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1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor

R. Richard Goehring,John F.W. Whitehead,Kevin K Brown,Khondaker Islam, Xin Wen,Xiaoming Zhou,Zhengming Chen,Kenneth J. Valenzano,Wendy S. Miller,Shen Shan,Donald J. Kyle

Bioorganic & medicinal chemistry letters（2005）

Cited 19|Views0
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Abstract
A series of 1,3-dihydro-2,1,3-benzothiadiazol-2,2-diones (I) and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones (II) were prepared. While the five-member ring series (I) did not show good affinity for opioid receptors, the six-member ring series (II) exhibited extremely high affinity and selectivity for the NOP receptor and showed full agonist activity, as determined by stimulation of GTPγ[35S] binding.
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Receptor Activation
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