Date published: 2025-12-16

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Taltirelin (CAS 103300-74-9)

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Alternate Names:
TA 0910; Ceredist; N-[[(4S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl-L-prolinamide
Application:
Taltirelin is a synthetic thyrotropin-releasing hormone analog
CAS Number:
103300-74-9
Molecular Weight:
405.41
Molecular Formula:
C17H23N7O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Taltirelin is a synthetic thyrotropin-releasing hormone (TRH) analog. Displays ~ 30-100-fold more potent CNS activity and ~ 50-fold weaker endocrine activity than TRH. Both antinociceptive and neuroprotective. Taltirelin features modifications that help prevent rapid degradation and extend its duration of action. Taltirelin may act to stimulate the release of neurotransmitters. Taltirelin is used in research to understand the role of TRH and its analogs in neurobiology. It helps in studying how modifying the TRH peptide can change its interaction with TRH receptors and the subsequent biological effects.


Taltirelin (CAS 103300-74-9) References

  1. Diversity of thyrotropin-releasing hormone receptors in the pituitary and discrete brain regions of rats.  |  Asai, H., et al. 1999. Jpn J Pharmacol. 79: 313-7. PMID: 10230859
  2. Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice.  |  Urayama, A., et al. 2002. Life Sci. 72: 601-7. PMID: 12467901
  3. The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems.  |  Tanabe, M., et al. 2007. Br J Pharmacol. 150: 403-14. PMID: 17220907
  4. Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety.  |  Suzuki, M., et al. 1990. J Med Chem. 33: 2130-7. PMID: 2115588
  5. Reversal of hemorrhagic shock in rats using the metabolically stable thyrotropin-releasing hormone analog taltirelin hydrate.  |  Asai, H., et al. 2011. J Recept Signal Transduct Res. 31: 416-22. PMID: 22044177
  6. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor.  |  Thirunarayanan, N., et al. 2012. Front Endocrinol (Lausanne). 3: 120. PMID: 23087672
  7. Thyrotropin-releasing hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin actions in the CNS of mice.  |  Thirunarayanan, N., et al. 2013. Neuropsychopharmacology. 38: 950-6. PMID: 23303050
  8. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue.  |  Dougherty, JP., et al. 2017. Pharmacol Res. 124: 1-8. PMID: 28720519
  9. Intravenous and Intratracheal Thyrotropin Releasing Hormone and Its Analog Taltirelin Reverse Opioid-Induced Respiratory Depression in Isoflurane Anesthetized Rats.  |  Boghosian, JD., et al. 2018. J Pharmacol Exp Ther. 366: 105-112. PMID: 29674333
  10. TRH Analog, Taltirelin Improves Motor Function of Hemi-PD Rats Without Inducing Dyskinesia via Sustained Dopamine Stimulating Effect.  |  Zheng, C., et al. 2018. Front Cell Neurosci. 12: 417. PMID: 30555300
  11. TRH Analog, Taltirelin Protects Dopaminergic Neurons From Neurotoxicity of MPTP and Rotenone.  |  Zheng, C., et al. 2018. Front Cell Neurosci. 12: 485. PMID: 30618632
  12. A Comparison of Breathing Stimulants for Reversal of Synthetic Opioid-Induced Respiratory Depression in Conscious Rats.  |  Dandrea, KE. and Cotten, JF. 2021. J Pharmacol Exp Ther. 378: 146-156. PMID: 34021024
  13. β-Arrestin2 Is Critically Involved in the Differential Regulation of Phosphosignaling Pathways by Thyrotropin-Releasing Hormone and Taltirelin.  |  Drastichova, Z., et al. 2022. Cells. 11: PMID: 35563779
  14. Are thyrotropin-releasing hormone (TRH) and analog taltirelin viable reversal agents of opioid-induced respiratory depression?  |  Algera, MH., et al. 2022. Pharmacol Res Perspect. 10: e00974. PMID: 35621218
  15. Thyrotropin-releasing hormone analog as a stable upper airway-preferring respiratory stimulant with arousal properties.  |  Liu, WY., et al. 2022. J Appl Physiol (1985). 133: 1067-1080. PMID: 36135952

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Taltirelin, 1 mg

sc-204319
1 mg
$118.00

Taltirelin, 10 mg

sc-204319A
10 mg
$250.00