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HC-067047

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
HC-067047
Identifiers
  • 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
CAS Number
PubChemCID
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC26H28F3N3O2
Molar mass471.524 g·mol−1
3D model (JSmol)
  • CC1=C(C=C(N1CCCN2CCOCC2)C3=CC=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)F
  • InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33)
  • Key:NCZYSQOTAYFTNM-UHFFFAOYSA-N

HC-067047 is a drug which acts as a potent and selective antagonist for theTRPV4 receptor. It has been used to investigate the role of TRPV4 receptors in a number of areas, such as regulation of blood pressure, bladder function and some forms of pain, as well as neurological functions.[1][2][3][4][5][6][7]

See also

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References

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  1. ^Everaerts W, Zhen X, Ghosh D, Vriens J, Gevaert T, Gilbert JP, et al. (November 2010)."Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis".Proceedings of the National Academy of Sciences of the United States of America.107 (44):19084–9.Bibcode:2010PNAS..10719084E.doi:10.1073/pnas.1005333107.PMC 2973867.PMID 20956320.
  2. ^Li L, Yin J, Jie PH, Lu ZH, Zhou LB, Chen L, Chen L (November 2013)."Transient receptor potential vanilloid 4 mediates hypotonicity-induced enhancement of synaptic transmission in hippocampal slices".CNS Neuroscience & Therapeutics.19 (11):854–62.doi:10.1111/cns.12143.PMC 6493605.PMID 23826708.
  3. ^Zhang L, Papadopoulos P, Hamel E (October 2013)."Endothelial TRPV4 channels mediate dilation of cerebral arteries: impairment and recovery in cerebrovascular pathologies related to Alzheimer's disease".British Journal of Pharmacology.170 (3):661–70.doi:10.1111/bph.12315.PMC 3792003.PMID 23889563.
  4. ^Chen Y, Kanju P, Fang Q, Lee SH, Parekh PK, Lee W, et al. (December 2014)."TRPV4 is necessary for trigeminal irritant pain and functions as a cellular formalin receptor".Pain.155 (12):2662–72.doi:10.1016/j.pain.2014.09.033.PMC 4295825.PMID 25281928.
  5. ^Jie P, Hong Z, Tian Y, Li Y, Lin L, Zhou L, et al. (June 2015)."Activation of transient receptor potential vanilloid 4 induces apoptosis in hippocampus through downregulating PI3K/Akt and upregulating p38 MAPK signaling pathways".Cell Death & Disease.6 (6): e1775.doi:10.1038/cddis.2015.146.PMC 4669828.PMID 26043075.
  6. ^Dias FC, Alves VS, Matias DO, Figueiredo CP, Miranda AL, Passos GF, Costa R (August 2019). "The selective TRPV4 channel antagonist HC-067047 attenuates mechanical allodynia in diabetic mice".European Journal of Pharmacology.856 172408.doi:10.1016/j.ejphar.2019.172408.PMID 31129158.S2CID 167205459.
  7. ^Thapak P, Vaidya B, Joshi HC, Singh JN, Sharma SS (September 2020). "Therapeutic potential of pharmacological agents targeting TRP channels in CNS disorders".Pharmacological Research.159 105026.doi:10.1016/j.phrs.2020.105026.PMID 32562815.S2CID 219959586.
TRPA
Activators
Blockers
TRPC
Activators
Blockers
TRPM
Activators
Blockers
TRPML
Activators
Blockers
TRPP
Activators
Blockers
TRPV
Activators
Blockers
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