RV-I-29

RV-I-29 is a deuterated small molecule analogue of Compound 6, acting as a selective positive allosteric modulator (PAM) of α6 subunit-containing GABAA receptors (α6GABAARs). These receptors are highly expressed in the trigeminal ganglia, which serves as the sensory hub of the trigeminovascular system. By enhancing GABAergic transmission in the trigeminal ganglia, RV-I-29 inhibits trigeminovascular system activation, thereby reducing peripheral and central sensitization associated with migraine. In preclinical models, RV-I-29 has demonstrated the ability to ameliorate neuronal activation in the trigeminal cervical complex and prevent the depletion of calcitonin gene-related peptide (CGRP) in the dura mater. It is being developed as a potential novel pharmacotherapy for migraine with improved pharmacokinetic properties, such as a longer half-life, compared to its parent compound.

Other names

deuterated Compound 6