HC-070 mimicked the effects of Trpc5 deletion in Th+ARC neurons, reducing interburst intervals and eliminating prolactin-evoked long-lasting depolarization.
Proc Natl Acad Sci U S A. 2019 Jul 23;116(30):15236-15243
human TRPC1/TRPC5 heteromultimer expressing cells
1.3 nM
To assess the inhibitory effect of HC-070 on TRPC1/TRPC5 heteromultimers
PLoS One. 2018 Jan 31;13(1):e0191225
mouse TRPC5 (mTRPC5) expressing cells
0.55 nM
To assess the inhibitory effect of HC-070 on mTRPC5
PLoS One. 2018 Jan 31;13(1):e0191225
human TRPC4 (hTRPC4) expressing cells
46.0±3.9 nM
To assess the inhibitory effect of HC-070 on hTRPC4
PLoS One. 2018 Jan 31;13(1):e0191225
human TRPC5 (hTRPC5) expressing cells
9.3±0.9 nM
To assess the inhibitory effect of HC-070 on hTRPC5
PLoS One. 2018 Jan 31;13(1):e0191225
T-Rex-293-hTRPC4 cells
1-30 nM (Englerin A activation), 3-100 nM (GTPγS activation)
To assess the inhibitory potency of HC-070 on human TRPC4. Results showed concentration-dependent inhibition of TRPC4 current with IC50 values of 0.96 nM (Englerin A) and 5.72 nM (GTPγS).
Application of HC-070 mimicked the effects of Trpc5 deletion in Th+ARC neurons, reducing interburst intervals and eliminating prolactin-evoked long-lasting depolarization.
Proc Natl Acad Sci U S A. 2019 Jul 23;116(30):15236-15243
Mice
C57BL/6 mice
Oral
1 mg/kg
Single dose
To assess the effect of HC-070 in a CCK-4-induced anxiety model
PLoS One. 2018 Jan 31;13(1):e0191225
Rats
Mechanical hypersensitivity model
Intrathecal administration
19 ng
Single administration
HC-070 had no significant effect on netrin-1-induced mechanical hypersensitivity during both early and late phases
Int J Mol Sci. 2022 Jun 14;23(12):6629
Wistar rats
Conscious Wistar rats with exposed dentin
Intravenous injection
0.008 nmol/g (weight)
Single administration
To evaluate the effect of TRPC5 channel antagonist on cold stimulation-induced dentinal sensitivity, results showed HC-070 did not significantly reduce nociceptive scores.
Front Physiol. 2022 Dec 14;13:891759
Rats
Visceral pain models (TNBS-induced colonic hypersensitivity and partial restraint stress model) and neuropathic pain model (chronic constriction injury model)
Oral
3-30 mg/kg
Single dose
To evaluate the analgesic efficacy of HC-070 in rat visceral and neuropathic pain models. Results showed HC-070 significantly and dose-dependently attenuated TNBS-induced colonic hypersensitivity and had a significant anti-hypersensitivity effect in the established phase of the CCI model.
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