Related Products of 57060-88-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.57060-88-5, Name is Methyl 1,2,3,4-tetrahydroisoquinoline-3-carboxylate hydrochloride, molecular formula is C11H14ClNO2. In a Article,once mentioned of 57060-88-5
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile
Derivatives of peptides of the TIPP (Tyr-Tic-Phe-Phe; Tic = 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) family containing a guanidino (Guan) function in place of the N-terminal amino group were synthesized in an effort to improve their blood-brain barrier permeability. Unexpectedly, N-terminal amidination significantly altered the in vitro opioid activity profiles. Guan-analogues of TIPP-related delta opioid antagonists showed delta partial agonist or mixed delta partial agonist/mu partial agonist activity. Guanidinylation of the mixed mu agonist/delta antagonists H-Dmt-Tic-Phe-Phe-NH2 (DIPP-NH2) and H-Dmt- TicPsi[CH2NH]Phe-Phe-NH2 (DIPP-NH2[Psi]) converted them to mixed mu agonist/delta agonists. A docking study revealed distinct positioning of DIPP-NH2 and Guan-DIPP-NH2 in the delta receptor binding site. Lys3-analogues of DIPP-NH2 and DIPP-NH2[Psi] (guanidinylated or non-guanidinylated) turned out to be mixed mu/kappa agonists with delta antagonist-, delta partial agonist- or delta full agonist activity. Compounds with some of the observed mixed opioid activity profiles have therapeutic potential as analgesics with reduced side effects or for treatment of cocaine addiction.
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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem