Uses
OB-1 is a stomatin-like protein-3 (STOML3) oligomerization blocker. OB-1 is an effective inhibitor of the self-association of Stomatin, STOML1 and STOML2, but not podocin[1].
Biological Activity
OB-1 is an inhibitor of the oligomerization of Stomatin-like protein-3 (STOML3), which is a modulator of the mechanosensitive ion channel Piezo2. STOML3 requires oligomerization for its role as an endogenous regulator of the sensitivity of mechanosensitive Piezo ion channels in sensory neurons. By inhibiting this activity, OB-1 has been shown to reduce touch-evoked pain behavior in two mouse models of neuropathic pain.
in vivo
OB-1 (250-500 pmol per paw; s.c.; once) reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in mice[1].
OB-1 (250 pmol per paw; s.c.; once) alleviates painful diabetic neuropathy in mice[1].
| Animal Model: | C57Bl/6N mice[1] |
| Dosage: | 250-500 pmol per paw |
| Administration: | Subcutaneous injection, once |
| Result: | Over 40% of Aβ fibers (19/44) lacked a mechanosensitive receptive field, which was significantly different from that in vehicle-injected controls, where less than 7% (5/69 fibers) were found to be insensitive to mechanical stimuli. Reduced touch perception. Reversed tactile allodynia. |
| Animal Model: | Eight-week-old C57Bl/6 mice, Streptozotocin (HY-13753) model[1] |
| Dosage: | 250 pmol per paw |
| Administration: | Subcutaneous injection, once |
| Result: | Substantially reversed the mechanical hypersensitivity 4 h after treatment. |
References
[1] Wetzel C, et al. Small-molecule inhibition of STOML3 oligomerization reverses pathological mechanical hypersensitivity. Nat Neurosci. 2017 Feb;20(2):209-218. DOI:
10.1038/nn.4454
