HC-030031 is a TRPA1 selective antagonist. TRPA1 may play an important role in acute formalin and CFA induced pain. HC-030031 does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels. The selective TRPA1 antagonist HC-030031 can be used in cells or delivered to animals orally, by inhalation, or by injection. Oral administration of HC-030031 reduced AITC-induced nocifensive behaviors at a dose of 100 mg/kg in the rat. Moreover, oral HC-030031 (100 mg/kg) significantly reversed mechanical hypersensitivity in the more chronic models of Complete Freunds Adjuvant (CFA)-induced inflammatory pain and the spinal nerve ligation model of neuropathic pain.
|Source||Cancer Res (2013). Figure 1. HC-030031|
|Cell Lines||C57BL/6 mice|
|Incubation Time||60 minutes|
|Results||Systemic treatment with HC-030031 (300 mg/kg, i.g.) at day 7 after treatment with bortezomib (0.2 or 0.5 mg/kg, i.p.) completely but transiently reverted both mechanical hyperalgesia and cold allodynia|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 27 mg/mL|
TRPA1 mediates mechanical sensitization in nociceptors during inflammation.
Lennertz RC, et al. PLoS One. 2012;7(8):e43597. PMID: 22927999.
HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity.
Eid SR, et al. Mol Pain. 2008 Oct 27;4:48. PMID: 18954467.
TRPA1 mediates formalin-induced pain.
McNamara CR, et al. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30. PMID: 17686976.
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