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Chemical Structure : RGH-235
Catalog No.: PC-47094Not For Human Use, Lab Use Only.
RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.
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RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.
RGH-235 was an inverse agonist ([35S] GTPγS binding) and antagonist (pERK1/2 ELISA), showing favourable kinetics, inhibition of the imetit-induced dipsogenia and moderate effects on sleep-wake EEG.
RGH-235 stimulated neurotransmitter release both in vitro and in vivo.
RGH-235 was active in spontaneously hypertensive rats (SHR), and exhibited a robust pro-cognitive profile both in rodens (0.3-1 mg/kg).
| M.Wt | 466.666 | |
| Formula | C29H42N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Némethy Z, et al. Eur J Pharmacol. 2022 Feb 5;916:174621.
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