Taltirelin Inhibitor CAS No. 103300-74-9

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KI0760	Taltirelin	1 mg	$190
KI0760	Taltirelin	10 mg	$358

Chemical Characteristic

Product Name	Taltirelin
Synonyms	Ceredist, TA 0910
CAS No.	103300-74-9
Molecular Weight	405.41
Formula	C₁₇H₂₃N₇O₅
Chemical Name	(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
Smiles	N1(C(=O)N[C@@H](CC1=O)C(=O)NC(C(=O)N1[C@@H](CCC1)C(=O)N)Cc1[nH]cnc1)C
Chemical Structure

Biological activities

Taltirelin is a thyrotropin-releasing hormone (TRH) analog. Taltirelin exhibits higher binding affinity and signaling potency at mouse TRH-R2 than TRH-R1 in a model cell system. In vivo, taltirelin shortens sleep time with pentobarbital sedation in WT and R2ko mice by 44 and 49% and with ketamine/xylazine sedation by 66 and 55%, but has no effect in R1ko and R1/R2ko mice. Taltirelin also increases response latency by 65 and 70% in WT and R2ko mice, but has no effect in R1ko and R1/R2ko mice.^[1] Taltirelin binds to rat brain TRH receptors in vivo. Taltirelin (0.3 mg/kg) also has neuroprotective effects in transient brain ischemia of C57BL/6J mice induced by bilateral carotid artery occlusion (2VO).^[2] Systemic administration of 1.0 mg/kg taltirelin also markedly reduces mechanical allodynia in mice with inflammatory persistent pain induced by an injection of complete Freund's adjuvant into the hindpaw.^[3]

Protocols

In vivo: Taltirelin is dissolved in sterile saline.^[2]

References

[1] Thirunarayanan N, et al. Thyrotropin-Releasing Hormone Receptor Type 1 (TRH-R1), not TRH-R2, Primarily Mediates Taltirelin Actions in the CNS of Mice. Neuropsychopharmacology. 2012. [2] Urayama A, et al. Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice. Life Sci. 2002, 72(4-5): 601-607. [3] Eto K, et al. Taltirelin, a thyrotropin-releasing hormone analog, alleviates mechanical allodynia through activation of descending monoaminergic neurons in persistent inflammatory pain. Brain Res. 2011, 1414: 50-57.

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