HC-067047

Last updated
HC-067047
HC-067047 structure.png
Identifiers
  • 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
CAS Number
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
Formula C26H28F3N3O2
Molar mass 471.524 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 the TRPV4 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

References

  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.
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