Taltirelin is a thyrotropin-releasing hormone (TRH) analog, which mimics the physiological actions of TRH, but with a much longer half-life and duration of effects.
CAT No: 10-101-63
CAS No:103300-74-9
Synonyms/Alias:Taltirelin;103300-74-9;TA 0910;Taltirelin [INN];taltirelina;taltireline;Ceredist;TA-0910;taltirelinum;UNII-DOZ62MV6A5;DOZ62MV6A5;CCRIS 8513;DTXSID0043763;TALTIRELIN [MI];TALTIRELIN [MART.];TALTIRELIN [WHO-DD];(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;(S)-N-((S)-1-((S)-2-Carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide;DTXCID8023763;CHEBI:135653;(-)-N-(((S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-L-histidyl-L-prolinamide;(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;NCGC00181033-01;TALTIRELIN (MART.);L-Prolinamide, N-(((4S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-L-histidyl-;L-Prolinamide, N-((hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-L-histidyl-, (S)-;1-methyl-(S)-4,5-dihydroorotyl-L-histidyl-L-prolinamide;(1-methyl-4,5-dihydroorotyl)-histidyl-prolinamide;N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide;N-(((4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl)carbonyl)-L-histidyl-L-prolinamide;(4S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl-L-prolinamide acetate salt;(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;(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;Taltirelin acetate salt;(4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide;SCHEMBL194528;GTPL2143;CHEMBL2107016;SCHEMBL21219549;SCHEMBL22077031;LQZAIAZUDWIVPM-SRVKXCTJSA-N;BCPP000053;(S)-N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide;BCP02001;HY-B0596;Tox21_112682;AKOS015920135;AKOS015969113;FT27992;NCGC00381723-02;AC-23956;BT300131;Taltirelin acetate salt - Bio-X trade mark;CAS-103300-74-9;NS00123276;Q7680336;BRD-K93869735-001-01-1;(1-methyl-(s)-4,5-dihydroorotyl)-l-histidyl-l-prolinamide;
Taltirelin is a synthetic thyrotropin-releasing hormone (TRH) analog that exhibits enhanced pharmacological stability and potency compared to endogenous TRH. As a peptide compound, it is structurally designed to mimic and modulate the activity of TRH receptors, making it a valuable tool in neuroendocrine research. Its resistance to enzymatic degradation and selective receptor activation enable precise investigations into hypothalamic-pituitary-thyroid (HPT) axis regulation, neuropeptide signaling, and central nervous system (CNS) function. Researchers utilize taltirelin to probe the physiological and biochemical mechanisms underlying TRH-mediated pathways, supporting a broad spectrum of experimental applications in molecular endocrinology and neurobiology.
Neuroendocrine signaling studies: Taltirelin serves as a robust probe for dissecting TRH receptor-mediated signaling pathways within the central nervous system and peripheral tissues. Its enhanced receptor affinity and metabolic stability allow researchers to investigate the dynamics of TRH receptor activation, downstream intracellular signaling cascades, and the modulation of gene expression related to neuroendocrine functions. Through controlled experimental administration, it enables the study of feedback mechanisms governing the HPT axis and the physiological consequences of altered TRH signaling.
Peptide receptor pharmacology: In the context of receptor pharmacology, taltirelin is employed to characterize the binding properties, selectivity, and functional responses of TRH receptor subtypes. Its use facilitates comparative analyses with native TRH and other analogs, enabling differentiation of receptor subtype contributions to physiological processes. By providing a stable and potent agonist, taltirelin aids in the elucidation of receptor-ligand interactions, receptor desensitization, and signal transduction mechanisms relevant to peptide hormone action.
Neuropeptide research and CNS function: Researchers leverage taltirelin to explore the broader roles of TRH-like peptides in central nervous system activity, including neurotransmitter modulation, neuroprotection, and behavioral responses. Its application in in vitro and in vivo experimental models supports investigations into the interplay between neuropeptides and neural circuits, advancing understanding of cognitive, motor, and neuroendocrine integration. These studies contribute to the mapping of TRH analog functions beyond classical endocrine regulation.
Peptide stability and metabolism studies: Due to its resistance to peptidase degradation, taltirelin is frequently used in studies examining peptide stability, metabolic pathways, and enzymatic breakdown in biological systems. Its structural modifications provide a reference for designing and evaluating new peptide analogs with improved bioavailability and pharmacokinetic profiles. These investigations are essential for advancing peptide drug design and understanding the factors that influence peptide persistence and activity in complex biological environments.
Analytical method development: Taltirelin acts as a reliable standard or reference compound in the development and validation of analytical techniques for peptide quantification and detection. Its well-characterized properties make it suitable for calibrating chromatographic, mass spectrometric, and immunological assays aimed at measuring TRH analogs and related peptides in biological matrices. The use of taltirelin in such contexts ensures accurate, reproducible data generation, supporting rigorous quality control and methodological advancement in peptide research laboratories.
Taltirelin (TAL) is a thyrotropin-releasing hormone (TRH) analog that is approved for use in humans in Japan. In this study, we characterized TAL binding to and signaling by the human TRH receptor (TRH-R) in a model cell system. We found that TAL exhibited lower binding affinities than TRH and lower signaling potency via the inositol-1,4,5-trisphosphate/calcium pathway than TRH. However, TAL exhibited higher intrinsic efficacy than TRH in stimulating inositol-1,4,5-trisphosphate second messenger generation. This is the first study that elucidates the pharmacology of TAL at TRH-R and shows that TAL is a superagonist at TRH-R. We suggest the superagonism exhibited by TAL may in part explain its higher activity in mediating central nervous system effects in humans compared to TRH.
Thirunarayanan, N., Raaka, B. M., & Gershengorn, M. C. (2012). Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Frontiers in endocrinology, 3.
Rovatirelin ([1-[-[(4S,5S)-(5-methyl-2-oxo oxazolidin-4-yl) carbonyl]-3-(thiazol-4-yl)-l-alanyl]-(2R)-2-methylpyrrolidine) is a novel synthetic agent that mimics the actions of thyrotropin-releasing hormone (TRH). The aim of this study was to investigate the electrophysiological and pharmacological effects of rovatirelin on the central noradrenergic system and to compare the results with those of another TRH mimetic agent, taltirelin, which is approved for the treatment of spinocerebellar degeneration (SCD) in Japan. Rovatirelin binds to the human TRH receptor with higher affinity (Ki=702nM) than taltirelin (Ki=3877nM). Rovatirelin increased the spontaneous firing of action potentials in the acutely isolated noradrenergic neurons of rat locus coeruleus (LC). The facilitatory action of rovatirelin on the firing rate in the LC neurons was inhibited by the TRH receptor antagonist, chlordiazepoxide. Reduction of the extracellular pH increased the spontaneous firing of LC neurons and rovatirelin failed to increase the firing frequency further, indicating an involvement of acid-sensitive K+ channels in the rovatirelin action. In in vivo studies, oral administration of rovatirelin increased both c-Fos expression in the LC and extracellular levels of noradrenaline (NA) in the medial prefrontal cortex (mPFC) of rats. Furthermore, rovatirelin increased locomotor activity. The increase in NA level and locomotor activity by rovatirelin was more potent and longer acting than those by taltirelin. These results indicate that rovatirelin exerts a central nervous system (CNS)-mediated action through the central noradrenergic system, which is more potent than taltirelin. Thus, rovatirelin may have an orally effective therapeutic potential in patients with SCD.
Ijiro, T., Nakamura, K., Ogata, M., Inada, H., Kiguchi, S., Maruyama, K., ... & Ishibashi, H. (2015). Effect of rovatirelin, a novel thyrotropin-releasing hormone analog, on the central noradrenergic system. European journal of pharmacology, 761, 413-422.
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