Protein Information

Name TRPM8
Synonyms LTRPC 6; LTRPC6; Long transient receptor potential channel 6; TRPM 8; TRPM8; TRPP 8; TRPP8; Transient receptor potential cation channel subfamily M member 8…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
18667618 Fajardo O, Meseguer V, Belmonte C, Viana F: TRPA1 channels mediate cold temperature sensing in mammalian vagal sensory neurons: pharmacological and genetic evidence. J Neurosci. 2008 Jul 30;28(31):7863-75.

Thus, most cold-evoked responses were potentiated by cinnamaldehyde, menthol, icilin, and BCTC [4-(3-chloro-pyridin-2-yl)-piperazine-1-carboxylic acid (4-tert-butyl-phenyl)-amide], agonists of TRPA1, and were inhibited by ruthenium red, camphor, and HC03001 [2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropy lphenyl) acetamide].
The pharmacological response to TRPM8 and TRPA1 agonists and antagonists suggested that, unlike results observed in somatic tissues, TRPA1 is the major mediator of cold-evoked responses in vagal visceral neurons.
1(0,0,0,1) Details
17317754 Malkia A, Madrid R, Meseguer V, de la Pena E, Valero M, Belmonte C, Viana F: Bidirectional shifts of TRPM8 channel gating by temperature and chemical agents modulate the cold sensitivity of mammalian thermoreceptors. J Physiol. 2007 May 15;581(Pt 1):155-74. Epub 2007 Feb 22.

We show that cold-evoked TRPM8 responses are effectively suppressed by inhibitor compounds SKF96365, 4-(3-chloro-pyridin-2-yl)-piperazine-1-carboxylic acid (4-tert-butyl-phenyl)-amide (BCTC) and 1,10-phenanthroline.
90(1,1,1,10) Details
18458237 Sabnis AS, Shadid M, Yost GS, Reilly CA: Human lung epithelial cells express a functional cold-sensing TRPM8 variant. Am J Respir Cell Mol Biol. 2008 Oct;39(4):466-74. Epub 2008 May 5.

The TRPM8 variant was expressed primarily within endoplasmic reticulum membranes of lung epithelial cells and its activation was attenuated by thapsigargin, the cell-permeable TRPM8 antagonist N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide, and shRNA-induced suppression of TRPM8 expression.
89(1,1,1,9) Details
17135413 Madrid R, Donovan-Rodriguez T, Meseguer V, Acosta MC, Belmonte C, Viana F: Contribution of TRPM8 channels to cold transduction in primary sensory neurons and peripheral nerve terminals. J Neurosci. 2006 Nov 29;26(48):12512-25.

To dissect out the contribution of this cold- and menthol-gated, nonselective cation channel to cold transduction, we identified BCTC [N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide] as a potent and full blocker of recombinant TRPM8 channels.
14(0,0,1,9) Details