Montirelin stimulates the release of thyrotropin and prolactin. It is synthesized by the neurons in the paraventricular nucleus of the hypothalamus. After being released into the pituitary portal circulation, TRH (was called TRF) stimulates the release of TSH and PRL from the anterior pituitary gland.
CAT No: 10-101-64
CAS No:62305-91-3
Synonyms/Alias:CG 3703; CG-3703; CG3703; CNK 602A; CNK602A; CNK-602A; CNK 603; CNK603; CNK-603; NS-3; NS3; NS 3; PS 24; Montirelin; Montireline; Montirelinum; Montirelin; Montirelina; CCRIS 7571; CCRIS7571
Montirelin is a synthetic tripeptide compound that functions as a potent thyrotropin-releasing hormone (TRH) analog. Structurally related to endogenous TRH, Montirelin exhibits enhanced metabolic stability and bioactivity, making it a valuable tool in neuroendocrine research. Its ability to modulate the hypothalamic-pituitary-thyroid axis and interact with TRH receptors has positioned it as a critical reagent for probing the physiological and biochemical roles of TRH signaling. Researchers utilize Montirelin to investigate mechanisms of hormone release, neuroregulation, and peptide-receptor dynamics, highlighting its significance in both fundamental and applied biochemical studies.
Neuroendocrine signaling research: Montirelin is widely employed in studies aimed at elucidating the regulatory mechanisms of the hypothalamic-pituitary-thyroid axis. By acting as a stable TRH analog, it enables precise stimulation of thyrotropin (TSH) secretion from the anterior pituitary in experimental systems. This property allows researchers to dissect the feedback loops and signaling pathways involved in thyroid hormone homeostasis, supporting advanced investigations into endocrine regulation at the molecular and cellular levels.
Receptor pharmacology: As a selective agonist of TRH receptors, Montirelin is instrumental in characterizing receptor-ligand interactions and downstream signaling events. Its high affinity and resistance to rapid enzymatic degradation provide a reliable means to activate TRH receptor subtypes in vitro and in vivo. This facilitates detailed studies on receptor binding kinetics, signal transduction pathways, and the pharmacological profiling of novel modulators targeting the TRH system.
Peptide stability and metabolism studies: The enhanced metabolic stability of Montirelin compared to native TRH makes it an ideal model compound for investigating peptide degradation pathways and enzymatic processing in biological matrices. Researchers leverage its resistance to peptidases to assess the stability profiles of peptide therapeutics, optimize peptide design, and develop analytical methods for peptide quantification in complex samples.
Neurotransmitter release investigations: Montirelin has been shown to influence the release of various neurotransmitters, including acetylcholine and dopamine, through its modulatory effects on central nervous system pathways. Scientists use it to explore the cross-talk between neuropeptide and classical neurotransmitter systems, contributing to a deeper understanding of neuronal communication, synaptic plasticity, and the broader landscape of neurochemical regulation.
Peptide-based assay development: The well-characterized activity and specificity of Montirelin support its use as a standard or positive control in biochemical assays designed to measure TRH receptor activation, hormone secretion, or peptide-mediated signaling events. Its inclusion in assay development protocols enables the validation of experimental systems, the calibration of detection methods, and the benchmarking of new peptide analogs or receptor modulators, thereby enhancing the reliability and reproducibility of neuroendocrine research workflows.
The histaminergic tuberomamillary nucleus (TMN) controls arousal and attention and the firing of TMN neurons is state-dependent, active during waking, silent during sleep. Thyrotropin-releasing hormone (TRH) promotes arousal and combats sleepiness associated with narcolepsy. Single-cell RT-PCR (scRT-PCR) demonstrated variable expression of the two known TRH receptors in the majority of TMN neurons. TRH increased the firing rate of most (ca 70%) TMN neurons. This excitation was abolished in the presence of the TRH receptor antagonist chlordiazepoxide (50 μM). In the presence of tetrodotoxin TRH depolarized TMN neurons without changing their input resistance. This effect reversed at the potential typical for nonselective cation channels. The potassium channel blockers barium and cesium did not influence the TRH-induced depolarization. TRH effects were antagonized by inhibitors of the Na+/Ca2+ exchanger, KB-R7943 and benzamil. The frequency of spontaneous inhibitory GABAergic postsynaptic potentials was either increased (TTX-insensitive) or decreased (TTX-sensitive GABA release sites) by TRH, indicating a heterogeneous modulation of GABAergic inputs by TRH. Montirelin (TRH analogue, 1 mg/kg ip) induced waking in wild type mice but not in histidine decarboxylase knockout mice lacking histamine. Inhibition of histamine synthesis by (S)-α-fluoromethylhistidine blocked the arousal effect of montirelin in WT mice. We conclude, that direct excitation of rodent TMN neurons by TRH is receptor-mediated and demands activation of nonselective cation channels as well as electrogenic Na+/Ca2+ exchange. Our findings indicate a key role of histamine in TRH-induced arousal.
Parmentier, R., Kolbaev, S., Klyuch, B. P., Vandael, D., Lin, J. S., Selbach, O., ... & Sergeeva, O. A. (2009). Excitation of histaminergic tuberomamillary neurons by thyrotropin-releasing hormone. Journal of Neuroscience, 29(14), 4471-4483.
1. Emu oil in combination with other active ingredients for treating skin imperfections
2. Low bone turnover and low BMD in Down syndrome: effect of intermittent PTH treatment
3. Store-operated Ca2+ entry sustains the fertilization Ca2+ signal in pig eggs
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More