HC-067047

HC-067047
Identifiers
	IUPAC name 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide;
CAS Number	883031-03-6;
PubChem CID	2742550;
CompTox Dashboard (EPA)	DTXSID70372463 ;
Chemical and physical data
Formula	C26H28F3N3O2
Molar mass	471.524 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=C(N1CCCN2CCOCC2)C3=CC=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)F;
	InChI 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]

References

^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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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[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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Identifiers

IUPAC name 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
CAS Number	883031-03-6
PubChem CID	2742550
CompTox Dashboard (EPA)	DTXSID70372463
Chemical and physical data
Formula	C₂₆H₂₈F₃N₃O₂
Molar mass	471.524 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=C(C=C(N1CCCN2CCOCC2)C3=CC=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)F
InChI 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

See also

References