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Different Biological Targets for Resiniferatoxin and Phorbol 12-Myristate 13-Acetate¹

Department of Pharmacology, Harvard Medical School, Boston, Massachusetts 02115

The phorbol-related diterpene ester resiniferatoxin is at least 100-fold more inflammatory for the mouse ear than is the potent tumor promoter phorbol 12-myristate 13-acetate but is nonpromoting. We report here that resiniferatoxin is 100- to 1000-fold less active than is phorbol 12-myristate 13-acetate in in vitro assays with both chicken and mouse fibroblasts. These results suggest that resiniferatoxin and phorbol 12-myristate 13-acetate have different primary target sites (receptors) and provide further evidence that the fibroblast target may be homologous to that involved in promotion.

¹ This research was supported by Grant CA-22895 from the NIH.

² Predoctoral Fellow of the Pharmaceutical Manufacturers Association.

³ Fellow of the Medical Foundation, Boston. To whom requests for reprints should be addressed.

Received 7/30/79. Accepted 1/24/80.

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