Thyrotropinreleasing hormone agonists

The neuropeptide, thyrotropin-releasing hormone (TRH), modulates CNS function, including activation of the cholinergic system. TRH analogs that overcome the short plasma half-life (4-5 min) include DN-1417 24, orotirelin 25, montirelin, RX-77368 26, MK-771 27, azetirelin, and posatirelin 28.41 Taltirelin (TA-0910: 29) is a small-molecule TRH agonist, with improved potency (up to 300-fold, depending on the biological assay) and pharmacokinetics (plasma t1/2 b 3 h) introduced in Japan in 2000 for the treatment of spinocerebellar degeneration. In animals, it dose-dependently increased extracellular ACh, potentiated ACh-induced neuronal excitation in cortical neurons, and inhibited ACh-induced desensitization. Taltirelin improved MMSE scores in demented patients and is reportedly in trials for AD.

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