Taltirelin Acetate CAS 103300-74-9

Taltirelin Acetate CAS 103300-74-9 is a synthetic thyrotropin-releasing hormone (TRH) analog primarily used to improve ataxia symptoms in patients with spinocerebellar degeneration.

Taltirelin was the world's first approved direct-acting thyrotropin-releasing hormone (TRH). In addition to its endocrine effects, it also exerts certain central nervous system (CNS) effects, including increasing motor activity, antagonizing reserpine-induced hypothermia, and antagonizing pentobarbital-induced sleep.

Taltirelin (TA0910) is a TRH-R superagonist with an IC50 of 910 nM and an EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).

Taltirelin is a structurally modified TRH product. Pharmacological studies show that it exerts strong and sustained multiple effects on the central nervous system (CNS) via TRH receptors in the brain. Its excitatory effect on the CNS is 10–100 times stronger than TRH, and its duration of action is approximately 8 times longer. Its affinity for TRH receptors is about 1/11 that of TRH, resulting in weaker endocrine effects, but it is more stable in vivo. Furthermore, its effect on thyroid-stimulating hormone (TSH) release is 1/6–1/11 that of TRH. TSH release is regulated by a strong negative feedback system including thyroid hormones, exhibiting a strong effect on the central nervous system, but with less hormone-like activity, thus fewer side effects.