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  • Title: Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
    Author: Kopka IE, Lin LS, Jewell JP, Lanza TJ, Fong TM, Shen CP, Lao ZJ, Ha S, Castonguay LG, Van der Ploeg L, Goulet MT, Hagmann WK.
    Journal: Bioorg Med Chem Lett; 2010 Aug 15; 20(16):4757-61. PubMed ID: 20643546.
    Abstract:
    The design, synthesis, and binding activity of ring constrained analogs of the acyclic cannabinoid-1 receptor (CB1R) inverse agonist taranabant 1 are described. The initial inspiration for these taranabant derivatives was its conformation 1a, determined by (1)H NMR, X-ray, and molecular modeling. The constrained analogs were all much less potent than their acyclic parent structure. The results obtained are discussed in the context of a predicted binding of 1 to a homology model of CB1R.
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