2. Academic Validation
  3. Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor

Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor

  • Bioorg Med Chem Lett. 2002 Apr 22;12(8):1189-92. doi: 10.1016/s0960-894x(02)00127-0.
Mark E McDonnell 1,  Sui Po Zhang,  Adrienne E Dubin,  Scott L Dax
Affiliations

Affiliation

  • 1 Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA.
PMID: 11934585 DOI: 10.1016/s0960-894x(02)00127-0
Abstract

Using a 'directed' iodination procedure, novel iodo-resiniferatoxin congeners were synthesized from 4-acetoxy-3-methoxyphenylacetic acid and resiniferinol- 9,13,14-ortho-phenylacetate (ROPA). The 2-iodo-4-hydroxy-5-methoxyphenylacetic acid ester of resiniferinol 5 displayed high affinity binding (K(i)=0.71 nM) for the human vanilloid VR1 receptor and functioned as a partial agonist.

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