RGH-235 | H3R antagonist | Probechem Biochemicals

Chemical Structure : RGH-235

RGH-235 (RGH235)

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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Biological Activity

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).

Physicochemical Properties

M.Wt	466.666
Formula	C29H42N2O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(8R,9S,13S,14R,15S)-N-ethyl-13-methyl-3-(3-((S)-2-methylpyrrolidin-1-yl)propoxy)-17-oxo-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-15-carboxamide

References

1. Némethy Z, et al. Eur J Pharmacol. 2022 Feb 5;916:174621.

RGH-235 (RGH235)

Biological Activity

Physicochemical Properties

References

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