78664-73-0 Usage
Uses
Used in Neurodegenerative Disease Treatment:
Posatirelin is used as a therapeutic agent for the treatment of neurodegenerative diseases such as vascular dementia and Parkinson's disease. It aids in the recovery of cholinergic neurons and their projections to the cerebral cortex, which are often affected in these conditions.
Used in Seizure Management:
Posatirelin is also utilized as an anticonvulsant, helping to manage and reduce the frequency and severity of seizures in patients.
Used in Alzheimer's Disease Treatment:
In Alzheimer's disease patients, Posatirelin is used as a cognitive enhancer to improve intellectual performance, orientation, motivation, and memory. It has been well-tolerated in patients and has shown significant benefits compared to controls.
Used in Vascular Dementia Treatment:
For patients with vascular dementia, Posatirelin is used to enhance cognitive functions and overall brain health. It has been shown to provide significant improvements in intellectual performance, orientation, motivation, and memory, making it a valuable treatment option for this condition.
Pharmacological Study
Posatirelin is a TRH analogue. In a rat experimental model
of brain cholinergic deficit by lesion of the nucleus basalis
magnocellularis (nbM), posatirelin treatment rescued
cholinergic neurones of the nbM and their cholinergic
projections to the cerebral cortex (Sabbatini et al., 1998).
Posatirelin has been used in AD and VaD patients (Parnetti
et al., 1995, 1996). VaD patients treated with posatirelin
showed a significant improvement in intellectual performance,
orientation, motivation and memory as compared
to controls. The drug was well tolerated.
Check Digit Verification of cas no
The CAS Registry Mumber 78664-73-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,8,6,6 and 4 respectively; the second part has 2 digits, 7 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 78664-73:
(7*7)+(6*8)+(5*6)+(4*6)+(3*4)+(2*7)+(1*3)=180
180 % 10 = 0
So 78664-73-0 is a valid CAS Registry Number.
InChI:InChI=1/C17H28N4O4/c1-10(2)9-12(17(25)21-8-4-6-13(21)15(18)23)20-16(24)11-5-3-7-14(22)19-11/h10-13H,3-9H2,1-2H3,(H2,18,23)(H,19,22)(H,20,24)/t11-,12-,13-/m0/s1
78664-73-0Relevant articles and documents
Synthesis of Thyrotropin-Releasing Hormone Analogues. 2. Tripeptides Structurally Greatly Differing from TRH with High Central Nervous System Activity
Szirtes, Tamas,Kisfaludy, Lajos,Palosi, Eva,Szporny, Laszlo
, p. 1654 - 1658 (1986)
A new series of thyrotropin-releasing hormone (TRH) analogues, obtained by further modifications of our most potent central nervous system (CNS) stimulating neutral tripeptides at both termini, were synthesized by the pentafluorophenyl ester method and tested for CNS and thyrotropin (TSH) releasing activity.Replacement of pyroglutamic acid by pyro-2-aminoadipic acid, 2-oxoimidazolidine-4-carboxylic acid or γ-butyrolactone-γ-carboxylic acid and that of proline by pipecolic acid, thiazolidine-4-carboxylic acid, or homoproline in 2>- and 2>TRH led to tripeptides structurally widely different from TRH.In spite of this fact, 7 of the 17 analogues (1, 2, 8-10, 16, and 17) have stronger anticataleptic effect than TRH, with negligible or no hormonal potency.The highest CNS activity was achieved when pyroglutamic acid was replaced by pyro-2-aminoadipic acid at the N-terminus .A novel synthesis of L-2-aminoadipic acid suitable for large-scale preparation is also described.
