Taltirelin

Names

[ Name ]:
Taltirelin

[Synonym ]:
Taltirelin
(-)-N-[[(S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl-L-prolinamide
L-Prolinamide, N-[[(4S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl-
N-{[(4S)-1-Methyl-2,6-dioxohexahydro-4-pyrimidinyl]carbonyl}-L-histidyl-L-prolinamide
(4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
N-{[(4S)-1-Methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide
TA-0910
Taltirelin Acetate

Biological Activity

[Description]:

Taltirelin(TA0910), a novel orally active TRH analogue, binds to rat brain TRH receptors in vivo.Target: OthersTaltirelin(TA0910), a novel orally active TRH analogue, binds to rat brain TRH receptors in vivo. Effects of taltirelin hydrate (CAS 103300-74-9, TA-0910), a novel thyrotropin-releasing hormone (TRH) analog, on the cerebral monoamine systems, especially the release and turnover of dopamine (DA) in rat brain were compared with those of TRH by intraperitoneal administration. Taltirelin hydrate (1-10 mg/kg) increased the extracellular levels of DA and its metabolites, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the nucleus accumbens and corpus striatum for 3 h in a microdialysis study. taltirelin hydrate possesses not only an enhancing effect on DA release, but also a stimulating effect on the monoamine system [1]. Taltirelin selectively bound to TRH receptors and increased the spontaneous motor activity by a single administration, suggesting that the motor effect of taltirelin is mediated by TRH receptors [2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

[References]

[1]. Fukuchi, I., et al., Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain. Arzneimittelforschung, 1998. 48(4): p. 353-9.

[2]. Asai, H., et al., Lack of behavioral tolerance by repeated treatment with taltirelin hydrate, a thyrotropin-releasing hormone analog, in rats. Pharmacol Biochem Behav, 2005. 82(4): p. 646-51.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Melting Point ]:
72-75°

[ Molecular Formula ]:
C₁₇H₂₃N₇O₅

[ Molecular Weight ]:
405.408

[ Exact Mass ]:
405.176056

[ PSA ]:
170.59000

[ LogP ]:
-4.09

[ Index of Refraction ]:
1.612

[ Storage condition ]:
2-8℃

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TW3578050

CAS REGISTRY NUMBER :: 103300-74-9

LAST UPDATED :: 199212

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C17-H23-N7-O5.4H2-O

MOLECULAR WEIGHT :: 477.55

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1590 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 33,2130,1990