Sequence: (1-methyl-4,5-dihydroorotyl)- His-Pro-NH2
Molecular Weight: 405.4091g/mol
Peptide purity: greater than 98%
Other details: No TFA Salt
Storage: Lyophilized peptide must be stored at -20°C and peptide solution at 4°C.
Taltirelin has good oral and excellent subcutaneous bioavailability.
Taltirelin has been marketed primarily for its effiacy as an Anti-Spinocerebellar Degeneration Agent. Taltirelin is a biased superagonist at TRH-R1 with a unique profile of efficacy.
One of the first cited studies back in 2002 shows this chemical, taltirelin, to be neuroprotective. This effect was exerted even with models of ischemia and other conditions that are hard to treat.
However, studies on it's neuroprotective, and moreover, pro-cognitive / nootropic effects date back to 1997; where it was demonstrated to have ameliorated consiousness impairment, memory impairment and motor dysfunction in several models. In 2007, a much larger study showed taltirelin to be a potent antinociceptive (pain relieving) ) as well, an effect at least partly, but certainly not solely, dependent on the indirect activation of serotonin 5-HT A receptors.
The larger wonders of this chemical began in 2013,with tests showing marvelous anti-depressant effects and even more significant, the demonstrations of it being almost unprecedented, and even comparable to methamphetamine (but not dangerous and without adverse events) in inducing/increasing dopamine release.
It was also demonstrated to have acute and chronic memory enhancement effects and could ameliorate memory impairment on a central hypothalamic level and by directly modulating cholinergic neurotransmission in the hippocampus, a brain area largely involved with spatial, active and declarative memory.
An anti-ataxic effect of taltirelin was noted as well - an effect that probably has to do with NMDA-glutamate receptor modulation/activation, as this benefit was blocked by an NMDA-antagonist; MK-801.
Taltirelin was also revealed to have nootropic. Brain cells and synapses increasing and this occurred at the molecular and central level. The most profound effects were seen in the spinal cord, though it was also noted to reverse nerve damage in other tissues/brain regions.
Taltirelin's effects on Neurotransmission:
• Taltirelin increases extracellular levels of acetylcholine in the hippocampus, but modulates turnover if levels are already high (potentially protecting against excesses of ACh as well).
• Taltirelin increases noradrenaline in the hypothalamus.
• Taltirelin super-potently increases dopamine release in the striatum and nucleus accumbens, which are area's involved in motivation and as such this is likely the responsible action for it's pungent anti-depressant effects.
• The compound also can regulate/increase serotonin levels in the brain stem. nucleus accumbens and striatum.
• Taltirelin may increase neurite outgrowth via distinct modulation of neurotrophic factors and via positive effects on blood flow.
In summary, Taltirelin has demonstrated the following effects/benefits:
• As an anti-depressant.
• As a nootropic.
• Ameliorating memory deficits, and increasing retention.
• As a novel analgesic/pain reliever.
• As a stimulant, with motivation increasing effects.
• Regenerating spinal cord nerves and treating spinal muscular atrophy.
• Rapidly increasing dopamine, noradrenaline, serotonin and acetylcholine.
• Amelioration of Autism Spectrum Diorder (ASD) and Obsessive-Compulsive Disorder (OCD) conditions.
• Fosters a superior state of arousal and vigilance.
• Increases cerebral metabolism and blood flow.
Some suggested clinical indications for TRH analogs:
• Depression, especially accompanied by hypersomnolence
• Chronic fatigue syndromes
• Excessive daytime sleepiness (including narcolepsy), neurasthenia,
• and lethargy
• Sedation secondary to drugs, chemotherapy, or radiation therapy
• Sedative intoxication/respiratory distress (ER setting)
• Recovery from general anesthesia
• Attention deficit/hyperactive disorder
• Disturbances of circadian rhythm (e.g. jet lag)
• Bipolar affective disorder as a mood stabilizer
• Anxiety disorders
• Alzheimer’s disease and other dementias with cognition deficits
• Seizure disorders
• Motor neuron disorders
• May be particularly effective as adjunctive therapy
T. Nakamura et al., "Taltirelin improves motor ataxia independently of monoamine levels in rolling mouse nagoya, a model of spinocerebellar atrophy" [PubMed]
K. Eto el al., "Taltirelin, a thyrotropin-releasing hormone analog, alleviates mechanical allodynia through activation of descending monoaminergic neurons in persistent inflammatory pain" [PubMed]
A. Urayama 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" [PubMed]
M. Yamamura et al., "Synthesis and pharmacological action of TRH analog peptide (Taltirelin)" [PubMed]
I. Fukuchi et al., "Effects of taltirelin hydrate (TA-0910), a novel thyrotropin-releasing hormone analog, on in vivo dopamine release and turnover in rat brain" [PubMed]
W.M. Brown "Taltirelin (Tanabe Seiyaku)" [PubMed]
Wen-Ying Liu et al., "Differential activating effects of thyrotropin-releasing hormone and its analog taltirelin on motor output to the tongue musculature in vivo" [PubMed]
C. Zheng et al., "TRH Analog, Taltirelin Protects Dopaminergic Neurons From Neurotoxicity of MPTP and Rotenone" [PubMed]
This product is intendend for lab research and development use only. These studies are performed outside of the body. This product is not medicines or drugs and has not been approved by the FDA or EMA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law. This product should only be handled by licensed, qualified professionals.
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