TRH analogs

Scheme 45 Synthesis of a TRH analog building block by anodic N-a-methoxylation.

Kabayama Y, Kato Y, Shimatsu A, Yanaihara N, Imura H (1986) Stimulation by gastrin-releasing peptide, neurotensin and DN1417, a novel TRH analog, of dopamine and norepinephrine release from perifused rat hypothalamic fragments in vitro. Brain Res 572 394-399. 

TRH Analogs. A similar strategy was used 56-359) for the CNS delivery of a thyrotropin-releasing hormone (TRH, Glp-His-Pro) analog (Glp-Leu-Pro) in which histidine (His ) was replaced with leucine (Leu )to... 

Selection of a suitable spacer proved also important for the efficacy of TRH-CDSs as measured by the decrease in the barbiturate-induced sleeping time in mice, an interesting and well-documented effect of this neuropeptide (425,426). After i.v. administration of 15 jLtmol/kg, the Leu -TRH analog itself produced only a slight decrease of 17 + 7% compared to the vehicle control. Equimolar doses of the CDS compounds with Pro, Pro-Pro, and Pro-Ala spacers produced statistically significant (p < 0.05) decreases of 47 6%, 51 7%, and 56 4%, respectively (358). Treatment with a TRH-CDS also significantly improved memory-related behavior in a passive-avoid-... 

Faden Al, Fox GB, Fan L, Araldi GL, Qiao L, Wang S, Kozikowski AP (1999) Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents. Am J Physiol 277 R1196-R1204... 

Drug Design and the Receptor-Bound Conformation of Thyrotropin Releasing Hormone (TRH) Design and Synthetic Approaches Towards Rigid TRH Analogs. 

---