3 documents found, page 1 of 1
Correlation between membrane translocation and analgesic efficacy in kyotorphin...
Serrano, Isa D.; Ramu, Vasanthakumar G.; Pinto, Antónia R. T.; Freire, João M.; Tavares, Isaura; Heras, Montserrat; Bardaji, Eduard R.Amidated kyotorphin (L-Tyr-L-Arg-NH2; KTP-NH2) causes analgesia when systemically administered. The lipophilic ibuprofen-conjugated derivative of KTP-NH2 has improved analgesic efficacy. However, fast degradation by peptidases impacts negatively in the pharmacodynamics of these drugs. In this work, selected derivatives of KTP and KTP-NH2 were synthesized to combine lipophilicity and resistance to enzymatic degr...
The mechanisms and quantification of the selective permeability in transport ac...
Serrano, Isa D.; Freire, João M.; Carvalho, Miguel V.; Neves, Mafalda; Melo, Manuel N.; Castanho, Miguel A. R. B.This paper addresses the mechanisms behind selective endothelial permeability and their regulations. The singular properties of each of the seven blood-tissues barriers. Then, it further revisits the physical, quantitative meaning of permeability, and the way it should be measured based on sound physical chemistry reasoning and methodologies. Despite the relevance of permeability studies one often comes across ...
Drug–lipid interaction evaluation : why a 19th century solution?
Ribeiro, Marta M. B.; Melo, Manuel N.; Serrano, Isa D.; Santos, Nuno C.; Castanho, Miguel A. R. B.The affinity of a drug candidate for a biological membrane (its lipophilicity) is closely related to the pharmacologically crucial events of absorption, biodistribution, metabolization and excretion. The evolution of knowledge of biological membranes during the past two decades contrasts with the rudimentary parameter most commonly used to assess lipophilicity: Po/w, the octanol–water partition coefficient. Po/...