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.

Diabetes Sustenance

Diabetes Sustenance

Get All The Support And Guidance You Need To Be A Success At Dealing With Diabetes The Healthy Way. This Book Is One Of The Most Valuable Resources In The World When It Comes To Learning How Nutritional Supplements Can Control Sugar Levels.

Get My Free Ebook

Post a comment