849461-91-2

TMPH Hydrochloride is a potent inhibitor of neuronal AChRs. Therapeutic agent potentially used for the treatment of this progressive neurodegenerative disease such as globoid cell leukodystrophy (GLD) or Krabbe disease.

2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH) is a potent inhibitor of neuronal nicotinic receptors. Evaluation of nicotinic acetylcholine receptor (nAChR) subunits expressed in Xenopus laevis oocytes indicated th at TMPH can produce a potent and long-lasting inhibition of neuronal nAChR formed by the pairwise combination of the most abundant neuronal alpha (i.e.alpha3 and alpha4) and beta subunits (beta2 and beta4)with relatively little effectbecause of rapid reversibility of inhibitionon muscle-type (alpha1beta1gammadelta) or alpha7 receptors. Howeverthe inhibition of neuronal beta subunit-containing receptors was also decreased if any of the nonessential subunits alpha5alpha6or beta3 were coexpressed. This decrease in inhibition is shown to be associated with a single amino acid present in the second transmembrane domain of these subunits. TMPH abilitty to relate the diverse central nervous system effects to specific nAChR subtypes makes it a useful tool for stud