HC-067047

HC-067047
HC-067047
HC-067047 structure.png
식별자
  • 2-메틸-1-(3-모르포린-4-일프로필)-5-페닐-N-[3-(트리플루오로메틸)페닐]피롤-3-카르복사미드
CAS 번호
PubChem CID
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C26H28F3N3O2
몰 질량471.524 g/120−1
3D 모델(JSmol)
  • CC1=C(C=C(N1CCN2CCCC2)C3=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)f
  • InChI=1S/C26H28F3N3O2/c1-19-23(25)30-22-10-5-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)126-16-13-13-34
  • 키: NCZYSQOTAYFTNM-UHFFFAOYSA-N

HC-067047은 TRPV4 수용체에 대한 강력한 선택적 길항제 역할을 하는 약물이다.그것은 혈압, 방광 기능 및 통증의 일부 형태뿐만 아니라 신경 [1][2][3][4][5][6][7]기능 조절과 같은 많은 영역에서 TRPV4 수용체의 역할을 조사하는데 사용되어 왔다.

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레퍼런스

  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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