Search

Your search keyword '"Polymethylene teraamine derivative"' showing total 2 results
Start Over Descriptor "Polymethylene teraamine derivative"
2 results on '"Polymethylene teraamine derivative"'

1. In vitro and in vivo evaluation of polymethylene tetraamine derivatives as NMDA receptor channel blockers.

Author

Saiki, Ryotaro, Yoshizawa, Yuki, Minarini, Anna, Milelli, Andrea, Marchetti, Chiara, Tumiatti, Vincenzo, Toida, Toshihiko, Kashiwagi, Keiko, and Igarashi, Kazuei

Subjects
*POLYMETHYLENE, *METHYL aspartate receptors, *STILBENE, *XENOPUS, *THROMBOSIS, *INFARCTION
Abstract

Abstract: The biological activities of six symmetrically substituted 2-methoxy-benzyl polymethylene tetraamines (1–4) and diphenylethyl polymethylene tetraamines (5 and 6) as N-methyl-d-aspartate (NMDA) receptor channel blockers, were evaluated in vitro and in vivo. Although all compounds exhibited stronger channel block activities in comparison to memantine in Xenopus oocytes voltage clamped at −70mV, only compound 2 (0.4mg/kg intravenous injection) decreased the size of brain infarction in a photochemically induced thrombosis model mice at the same extent of memantine (10mg/kg intravenous injection). Other compounds (1, 3, 4, 5 and 6) did not decrease the size of brain infarction significantly due to the limited injection doses. The present study suggests that compound 2 could represent a valuable lead compound to design low toxicity polyamines for clinical use against stroke. [Copyright &y& Elsevier]

Published
2013
Full Text
View/download PDF

2. In vitro and in vivo evaluation of polymethylene tetraamine derivatives as NMDA receptor channel blockers

Author

Ryotaro Saiki, Yuki Yoshizawa, Anna Minarini, Kazuei Igarashi, Keiko Kashiwagi, Andrea Milelli, Toshihiko Toida, Vincenzo Tumiatti, Chiara Marchetti, Ryotaro Saiki, Yuki Yoshizawa, Anna Minarini, Andrea Milelli, Chiara Marchetti, Vincenzo Tumiatti, Toshihiko Toida, Keiko Kashiwagi, and Kazuei Igarashi

Subjects
Clinical Biochemistry, Xenopus, NMDA receptor channel blocker, Pharmaceutical Science, Pharmacology, Receptors, N-Methyl-D-Aspartate, Biochemistry, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Memantine, In vivo, Drug Discovery, Polyamines, medicine, Animals, Channel blocker, Molecular Biology, Dose-Response Relationship, Drug, Molecular Structure, biology, Chemistry, Organic Chemistry, Thrombosis, biology.organism_classification, Polymethylene tetraamine, In vitro, Disease Models, Animal, Drug Design, Molecular Medicine, NMDA receptor, Polymethylene teraamine derivative, Lead compound, medicine.drug
Abstract

The biological activities of six symmetrically substituted 2-methoxy-benzyl polymethylene tetraamines (1–4) and diphenylethyl polymethylene tetraamines (5 and 6) as N-methyl- d -aspartate (NMDA) receptor channel blockers, were evaluated in vitro and in vivo. Although all compounds exhibited stronger channel block activities in comparison to memantine in Xenopus oocytes voltage clamped at −70 mV, only compound 2 (0.4 mg/kg intravenous injection) decreased the size of brain infarction in a photochemically induced thrombosis model mice at the same extent of memantine (10 mg/kg intravenous injection). Other compounds (1, 3, 4, 5 and 6) did not decrease the size of brain infarction significantly due to the limited injection doses. The present study suggests that compound 2 could represent a valuable lead compound to design low toxicity polyamines for clinical use against stroke.

Published
2013
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results