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TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: compounds pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development

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Phase 1 trial data included groups that started directly at higher doses, and while efficacy was not compromised, GI side effect rates nearly doubled compared to the gradual approach

The remaining 14 cells (66.7%) did not respond to Ex-4 (0.10.3 mV, n =14)