Taltirelin

Modify Date: 2024-01-02 14:46:17

Taltirelin Structure
Taltirelin structure
Common Name Taltirelin
CAS Number 103300-74-9 Molecular Weight 405.408
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C17H23N7O5 Melting Point 72-75°
MSDS N/A Flash Point N/A

 Use of Taltirelin


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].

 Names

Name Taltirelin
Synonym More Synonyms

 Taltirelin 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
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.

 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

 Synonyms

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