Structural basis of species-dependent differential affinity of 6-alkoxy-5-aryl-3-pyridinecarboxamide cannabinoid-1 receptor antagonists
Alkoxy-5-aryl-3-pyridincarboxamides, including the brain-penetrant compound 14g [5-(4-
chlorophenyl)-6-(cyclopropylmethoxy)-N-[(1R, 2R)-2-hydroxy-cyclohexyl]-3-
pyridinecarboxamide] and its peripherally restricted analog 14h [5-(4-chlorophenyl)-N-[(1R,
2R)-2-hydroxycyclohexyl]-6-(2-methoxyethoxy)-3-pyridinecarboxamide], have been recently
introduced as selective, high-affinity antagonists of the human cannabinoid-1 receptor (hCB
1 R). Binding analyses revealed two orders of magnitude lower affinity of these compounds …
chlorophenyl)-6-(cyclopropylmethoxy)-N-[(1R, 2R)-2-hydroxy-cyclohexyl]-3-
pyridinecarboxamide] and its peripherally restricted analog 14h [5-(4-chlorophenyl)-N-[(1R,
2R)-2-hydroxycyclohexyl]-6-(2-methoxyethoxy)-3-pyridinecarboxamide], have been recently
introduced as selective, high-affinity antagonists of the human cannabinoid-1 receptor (hCB
1 R). Binding analyses revealed two orders of magnitude lower affinity of these compounds …
