Taltirelin CAS 103300-74-9

Taltirelin - Names and Identifiers

Name	Taltirelin
Synonyms	TA 0910 Taltirelin Ceredist, TA-0910 Taltirelin interMediate TALTIRELIN INTERMEDIATES Taltirelin Acetate,TA-0910 L-Prolinamide,(4S)-hexahydro-1-methyl- 2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl- (4S)-Hexahydro-1-Methyl-2,6-dioxo-4-pyriMidinecarbonyl-L-histidyl- N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide L-Prolinamide, N-[(hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl]-L-histidyl-, (S)- L-Prolinamide, N-[[(4S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl- (9CI) (4S)-N-[(2S)-1-[(2S)-2-Carbamoylpyrrolidin-1-yl]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
CAS	103300-74-9
InChI	InChI=1/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1

Taltirelin - Physico-chemical Properties

Molecular Formula	C17H23N7O5
Molar Mass	405.41
Density	1.447±0.06 g/cm3(Predicted)
Melting Point	72-75°
Specific Rotation(α)	25D -13.6° (c = 1 in water)
pKa	9.32±0.40(Predicted)
Storage Condition	Store at +4°C
Refractive Index	1.611

Taltirelin - Reference Information

, it was successfully developed by Mitsubishi Pharmaceutical Co., Ltd., Japan, and its trade name is taltielin. It belongs to the 3.1 class of new chemical drugs. At present, it is the most effective drug for improving the movement disorder of patients with spinocerebellar degeneration.
Taltirelin is the first approved oral thyrotropin-releasing hormone (TRH) in the world, it may also exert certain central nervous system (CNS) effects, including increased locomotor activity, antagonism of liserpin-induced hypothermia, and antagonism of pentobarbital-induced sleep. The variety was developed by Mitsubishi AG, Japan, and was first launched in Japan in September 2000. It is used to improve ataxia in patients with spinocerebellar degeneration. Spinocerebellar ataxia (SCAs), formerly known as autosomal dominant ataxia, is a group of chronic degenerative diseases of the central nervous system with ataxia and poor differentiation as the main clinical manifestations. Before September 2000, thyrotropin-releasing hormone (TRH) injection was the only drug used to treat this disease. Tatrierelin is a structural modification drug of TRH. Pharmacological studies have shown that this product produces strong and lasting multiple effects on the CNS via brain TRH receptors. The Excitatory effect of this product on CNS is 10~100 times stronger than TRH, and the duration of action is about 8 times longer than TRH. The affinity of this product to TRH receptor is about 1/11 of TRH, so the endocrine effect of this product is weaker than TRH, but this product is more stable than TRH in vivo. In addition, the effect of this product on the release of thyroid stimulating hormone (TSH) is 1/6-1/11 of TRH, and the release of TSH is regulated by a strong negative feedback system including thyroid hormone, has a strong effect on the central nervous system, but at the same time its hormone-like effect is small, so less side effects. Adverse reactions were mainly digestive system reactions, including Vomit, Nausea and stomach discomfort. All adverse reactions were mild to moderate and disappeared during treatment and/or after drug withdrawal.

oral thyrotropin-releasing hormone
biological activity	taltielin (TA0910) is a thyrotropin-releasing hormone receptor (TRH-R) superagonist, the IC50 value was 910 nM and the EC50 value for stimulating an increase in cytosolic Ca2 concentration (Ca2 release) was 36 nM.
Target	IC50: 910 nM