1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Quality Control of 1H-Benzo[d][1,2,3]triazol-1-amine
Nonclinical pharmacokinetics, disposition, and drug-drug interaction potential of a novel D-amino acid peptide agonist of the calcium-sensing receptor AMG 416 (Etelcalcetide) was written by Subramanian, Raju;Zhu, Xiaochun;Kerr, Savannah J.;Esmay, Joel D.;Louie, Steven W.;Edson, Katheryne Z.;Walter, Sarah;Fitzsimmons, Michael;Wagner, Mylo;Soto, Marcus;Pham, Roger;Wilson, Sarah F.;Skiles, Gary L.. And the article was included in Drug Metabolism & Disposition in 2016.Quality Control of 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:
AMG 416 (etelcalcetide) is a novel synthetic peptide agonist of the calcium-sensing receptor composed of a linear chain of seven D-amino acids (referred to as the D-amino acid backbone) with a D-cysteine linked to an L-cysteine via a disulfide bond. AMG 416 contains four basic D-arginine residues and is a +4 charged peptide at physiol. pH with a mol. weight of 1048.3 Da. The pharmacokinetics (PK), disposition, and potential of AMG 416 to cause drug-drug interaction were investigated in nonclin. studies with two single 14C-labels placed either at a potentially metabolically labile acetyl position or on the D-alanine next to D-cysteine in the interior of the D-amino acid backbone. After i.v. dosing, the PK and disposition of AMG 416 were similar in male and female rats. Radioactivity rapidly distributed to most tissues in rats with intact kidneys, and renal elimination was the predominant clearance pathway. No strain-dependent differences were observed In bilaterally nephrectomized rats, minimal radioactivity (1.2%) was excreted via nonrenal pathways. Biotransformation occurred primarily via disulfide exchange with endogenous thiol-containing mols. in whole blood rather than metabolism by enzymes, such as proteases or cytochrome P450s; the D-amino acid backbone remained unaltered. A substantial proportion of the plasma radioactivity was covalently conjugated to albumin. AMG 416 presents a low risk for P 450 or transporter-mediated drug-drug interactions because it showed no interactions in vitro. These studies demonstrated a 14C label on either the acetyl or the D-alanine in the D-amino acid backbone would be appropriate for clin. studies. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Quality Control of 1H-Benzo[d][1,2,3]triazol-1-amine).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Quality Control of 1H-Benzo[d][1,2,3]triazol-1-amine
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics