| Bioactivity | JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine[1][2]. | ||||||||||||
| Invitro | JNJ-17203212 (0.5 μM) potently inhibits imperatorin-induced TRPV1 activation (Ca2+ increases) in TRPV1-expressing HEK cells[1]. | ||||||||||||
| In Vivo | JNJ-17203212 (0.3 mg/kg; i.v.) dose-dependently reduces inflammatory soup (IS)-induced the immediate early gene c-fos expression[2].JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner[2]. Animal Model: | ||||||||||||
| Name | JNJ-17203212 | ||||||||||||
| CAS | 821768-06-3 | ||||||||||||
| Formula | C17H15F6N5O | ||||||||||||
| Molar Mass | 419.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Xingjuan Chen, et al. Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel.J Biol Chem. 2014 Apr 4; 289(14): 9600-9610. [2]. Jannis E Meents, et al. Two TRPV1 receptor antagonists are effective in two different experimental models of migraine. J Headache Pain. 2015; 16: 57. |