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 recognized for its enhanced stability and prolonged activity compared to endogenous TRH. Developed through advanced peptide engineering, Taltirelin demonstrates high affinity for the TRH receptor, making it a valuable research tool in neuroendocrinology and neuropharmacology. Its unique structural modifications confer improved resistance to enzymatic degradation, allowing for more sustained biological effects and reliable experimental outcomes. The compound is frequently utilized in laboratory settings to explore the physiological and molecular mechanisms underlying TRH receptor activation, neurotransmitter modulation, and central nervous system (CNS) regulation. With its robust pharmacological profile, Taltirelin serves as a versatile molecule for investigating a range of neurological and endocrine pathways.
Neuroscience Research: Taltirelin is extensively employed in neuroscience research to elucidate the role of TRH signaling in the central nervous system. By selectively activating TRH receptors, researchers can dissect the pathways involved in neurotransmitter release, synaptic plasticity, and neuronal excitability. Its ability to cross the blood-brain barrier and exert central effects enables detailed studies on brain regions implicated in arousal, mood regulation, and cognitive function. Such investigations contribute to a deeper understanding of the neurobiological substrates of behavior and the potential for modulating CNS activity through TRH receptor pathways.
Endocrine System Studies: As a potent TRH analog, Taltirelin is instrumental in probing the hypothalamic-pituitary-thyroid (HPT) axis and its regulatory mechanisms. Scientists utilize it to stimulate the release of thyroid-stimulating hormone (TSH) from the anterior pituitary in in vitro and in vivo models, thereby mapping feedback loops and hormonal interactions within the endocrine system. This approach facilitates the exploration of thyroid hormone synthesis, secretion, and downstream metabolic effects, providing insights into both physiological and pathological states of thyroid function.
Neuroprotection Research: The neuroprotective properties of Taltirelin are a subject of growing interest, particularly in models of neurodegeneration and neuronal injury. Researchers investigate its capacity to modulate excitotoxicity, oxidative stress, and apoptotic pathways in neuronal cells. By leveraging its TRH receptor-mediated signaling, studies aim to uncover mechanisms that may preserve neuronal integrity and promote cell survival under adverse conditions. These findings have the potential to inform strategies for mitigating neuronal damage in various experimental contexts.
Fatigue and Motor Function Models: In preclinical studies, Taltirelin is used to assess its impact on fatigue and motor function, especially in animal models of neuromuscular disorders. Its stimulatory effects on the CNS are harnessed to evaluate improvements in locomotor activity, muscle strength, and endurance. By analyzing behavioral and physiological responses, researchers gain valuable data on the modulation of motor circuits and the interplay between central neurotransmitters and peripheral muscle function.
Signal Transduction Pathway Analysis: The compound also serves as a critical tool for dissecting intracellular signal transduction pathways triggered by TRH receptor activation. Scientists employ it to map downstream effectors, such as cyclic AMP (cAMP), protein kinase cascades, and gene expression profiles in various cell types. These studies are pivotal for identifying molecular targets and regulatory nodes within TRH-mediated signaling networks, advancing the broader understanding of peptide hormone action at the cellular level.
Metabolic Regulation Research: Taltirelin is increasingly utilized in metabolic studies to investigate its influence on energy balance, appetite control, and thermogenesis. By modulating TRH receptor activity, researchers examine alterations in feeding behavior, body weight, and metabolic rate in experimental models. This line of research provides novel perspectives on the integration of neuroendocrine signals governing metabolism and may reveal new avenues for addressing metabolic dysregulation in laboratory settings.
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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