Taltirelin Research

McMackin R, Price S, Slator GR, Hardiman O, Kelly JA

There is a pressing unmet clinical and health economic need for effective drugs to treat cognitive impairment that occurs in neurodegenerative diseases. JAK4D is a first-in-class thyrotropin releasing hormone (TRH) analogue that overcomes the pharmacological limitations of thyrotropin releasing h...

Ding K, Zhang Z, Niu J, Zhu M, Zhang J, Chen L et al.

Thyrotropin-releasing hormone (TRH) plays an important role in the regulation of emotion and cognition. However, whether TRH in the hippocampus participates in the development of post-traumatic stress disorder (PTSD)-like behaviors and the mechanisms involved remain unclear. Transcriptomic analys...

Zhu K, Meng L, Luo J, Wen T, Dan L, Wang Z et al.

Taltirelin, an orally effective thyrotropin-releasing hormone analog, significantly improves motor impairments in rat models of Parkinson's disease (PD) and enhances dopamine release within the striatum. However, the underlying mechanism remains unclear. In this study, a variety of in vivo and in...

Eto K, Ogata M, Kojima F, Ishibashi H

Itch is an unpleasant sensation that induces a desire to scratch. Chronic itch is accompanied by inflammatory skin diseases and causes repetitive scratching leading to tissue damage. The thyrotropin-releasing hormone analog taltirelin exerts analgesic effects on acute and chronic pain by activati...

Yamaoka M, Neshige S, Sasaki K, Maruyama H

A 54-year-old male presented with a two-year history of recurrent syncope. Although he was treated with droxidopa and amezinium metilsulfate, his syncope was drug-resistant. Blood tests, cardiac evaluation and brain computed tomography (CT) were unremarkable. As his Schellong test was positive, o...

Cho JW, Lee JY, Kim HJ, Kim JS, Park KW, Choi SM et al.

We conducted this study to assess the efficacy and safety of taltirelin hydrate (TH) in patients with ataxia due to spinocerebellar degeneration (SCD).Patients were randomly assigned to either the taltirelin group (5 mg orally, twice daily) or the control group. The primary endpoint was the chang...

Xia Y, Li X, Bie N, Pan W, Miao YR, Yang M et al.

Combination therapy is a promising therapeutic strategy to enhance the efficacy of immune checkpoint blockade (ICB); however, predicting drugs for effective combination is challenging. Here we developed a general data-driven method called CM-Drug for screening compounds that can boost ICB treatme...

Drastichova Z, Trubacova R, Novotny J

Thyrotropin-releasing hormone (TRH) is known to activate several cellular signaling pathway, but the activation of the TRH receptor (TRH-R) has not been reported to regulate gene transcription. The aim of this study was to identify phosphosignaling pathways and phosphoprotein complexes associated...

Aggarwal J, Ladha R, Liu WY, Liu H, Horner RL

Pharyngeal muscle activity and responsiveness are key pathophysiological traits in human obstructive sleep apnea (OSA) and strong contributors to improvements with pharmacotherapy. The thyrotropin-releasing hormone (TRH) analog taltirelin is of high pre-clinical interest given its neuronal-stimul...

Ishida N, Ono S, Suzuki R, Nojiri K, Ootsuki S, Zakoji N et al.

Drooling represents a common and noteworthy symptom in patients with intractable neuromuscular disease (IND) and cerebral palsy (CP) and can lead to poor quality of life (QOL) and higher incidence of death due to aspiration of saliva. Identifying the factors affecting drooling is crucial to impro...

Matsushima M, Yabe I

No disease-modifying therapy has been established for spinocerebellar degeneration and multiple system atrophy, and only symptomatic therapy is currently available. Taltirelin and protirelin are drugs covered by health insurance for cerebellar ataxia symptoms, and are expected to suppress the pro...

Liu WY, Ladha R, Liu H, Horner RL

Taltirelin is a stable, brain-penetrating thyrotropin-releasing hormone (TRH) analog with minimal endocrine activity and potential respiratory stimulant properties. Taltirelin's receptor target shows high differential expression at the hypoglossal motor nucleus, and local taltirelin microperfusio...

Ijiro T, Yaguchi A, Yokoyama A, Kiguchi S

Thyrotropin-releasing hormone (TRH) and the TRH mimetic taltirelin have been used in Japan for the treatment of spinocerebellar degeneration (SCD), a type of progressive ataxia. A TRH mimetic, rovatirelin, ameliorates ataxia symptoms in the rolling mouse Nagoya, a hereditary SCD model. The aim of...

Algera MH, Cotten JF, van Velzen M, Niesters M, Boon M, Shoham DS et al.

Opioid-induced respiratory depression (OIRD) is a potentially life-threatening complication of opioid consumption. Apart from naloxone, an opioid antagonist that has various disadvantages, a possible reversal strategy is treatment of OIRD with the hypothalamic hormone and neuromodulator thyrotrop...

Drastichova Z, Trubacova R, Novotny J

In recent years, thyrotropin-releasing hormone (TRH) and its analogs, including taltirelin (TAL), have demonstrated a range of effects on the central nervous system that represent potential therapeutic agents for the treatment of various neurological disorders, including neurodegenerative disease...

Algera MH, Cotten JF, van Velzen M, Niesters M, Boon M, Shoham DS et al.

Dandrea KE, Cotten JF

Potent synthetic opioids are an important cause of death in the United States' opioid epidemic, and a breathing stimulant may have utility in treating opioid overdose. We hypothesized that sufentanil-induced respiratory depression may be reversed by breathing stimulant administration. Using nose-...

Ijiro T, Yaguchi A, Yokoyama A, Abe Y, Kiguchi S

Rovatirelin is a newly synthetized thyrotropin-releasing hormone (TRH) analog. This study aimed to investigate the effect of rovatirelin on motor function using rolling mouse Nagoya (RMN), a mouse model of hereditary ataxia, and compare it with that of taltirelin, which is clinically used to trea...

Liu WY, Liu H, Aggarwal J, Huang ZL, Horner RL

Thyrotropin-releasing hormone (TRH) is produced by the hypothalamus but most brain TRH is located elsewhere where it acts as a neuromodulator. TRH-positive neurons project to the hypoglossal motoneuron pool where TRH receptor RNA shows a high degree of differential expression compared with the re...

Zheng C, Chen G, Tan Y, Zeng W, Peng Q, Wang J et al.

Dopaminergic neurons loss is one of the main pathological characters of Parkinson's disease (PD), while no suitable neuroprotective agents have been in clinical use. Thyrotropin-releasing hormone (TRH) and its analogs protect neurons from ischemia and various cytotoxins, but whether the effect al...