title: Bis (histidine) with N2 vehicle: an important skeleton for MR/chelation therapy.
abstract: Bis (histidine) ethylenediamine tetraacetic acid, EDTA-bis (amide) analog, has been synthesized starting from with EDTA bis-anhydride and protected histidine and evaluated in vitro as an important agent for MR and chelation therapy. The kinetic inertness of compound was analyzed by the exchange reactions with the essential metals of human body. The stability and protonation constants of the complexes formed between the ligand and M(3+) and M(2+) have been determined by pH potentiometry and spectrophotometry at 25 °C and constant ionic strength maintained with 0.10 m KCl. The in vivo stability and metabolite profile were confirmed in plasma and serum.
authors.affiliation: Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi, 110054, India.
authors.forename: Pooja
authors.initials: P
authors.lastname: Srivastava
authors.forename: Anjani K
authors.initials: AK
authors.lastname: Tiwari
authors.forename: Dipti Kakkar
authors.initials: DK
authors.lastname: Thukral
authors.forename: Vikas
authors.initials: V
authors.lastname: Kumar
authors.forename: Anil K
authors.initials: AK
authors.lastname: Mishra
mesh_terms: D000277:Adjuvants, Pharmaceutic; D000812:Anhydrides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002614:Chelating Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D056831:Coordination Complexes / Q000737:chemistry; D004492:Edetic Acid / Q000737:chemistry* / Q000494:pharmacology; D006639:Histidine / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D008807:Mice, Inbred BALB C; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis; D011817:Rabbits
chemical_list: D000277:Adjuvants, Pharmaceutic; D000812:Anhydrides; D002614:Chelating Agents; D056831:Coordination Complexes; D004364:Pharmaceutical Preparations; D006639:Histidine; D004492:Edetic Acid
keywords: MR vehicle; chelation; ethylenediamine tetraacetic acid; protonation constants; stability constant