Published November 2021 | Version v1
Journal article Metadata-only

Novel O-[11C]-methylated derivatives of the neprilysin inhibitor sacubitril: Radiosynthesis, autoradiography and plasma stability evaluation

Creators

  • 1. Institut de Génie Biomédical, Faculté de Médecine, Université de Montréal, Pavillon Paul-G. Desmarais, 2960 chemin de la Tour, Montréal, Québec H3T 1J4 (Canada)
  • 2. Laboratoire de Radiochimie et Cyclotron, Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montréal, Québec H2X 0A9 (Canada)
  • 3. Regroupement Cardio-vasculaire, Centre Hospitalier de l'Université de Montréal, 1051 Rue Sanguinet, Montréal, Québec H2X 3E4 (Canada)
  • 4. Laboratoire de Recherche @CoeurLab, Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montréal, Québec H2X 0A9 (Canada)
  • 5. Plateforme de Pharmacocinétique, Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montréal, Québec H2X 0A9 (Canada)
  • 6. Département de Radiologie, radio-oncologie et médecine nucléaire, Faculté de médecine, Université de Montréal, Pavillon Roger-Gaudry, 2900 boulevard Edouard Montpetit, Montréal, Québec H3T 1J4 (Canada)

Description

The O-[11C]methylated derivatives of the clinically used neprilysin inhibitor (NEPi) sacubitril ([11C]SacOMe, (2R,4S)-ethyl 5-([biphenyl]-4-yl)-4-(4-[11C]methoxy-4-oxobutanamido)-2-methylpentanoate) and LBQ657 ([11C]MeOLBQ, (2R,4S)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid [11C]methyl ester and [11C]LBQOMe, (2R,4S)-5-(biphenyl-4-yl)-4-[(4-[11C]methoxy-4-oxobutanamido)]-2-methylpentanoic acid) were evaluated to determine their potential as PET imaging tracers and investigate the effect of such labeling esterification on neprilysin (NEP) binding.

Availability note (English)

Available from http://dx.doi.org/10.1016/j.nucmedbio.2021.09.001

Additional details

Identifiers

DOI
10.1016/j.nucmedbio.2021.09.001;
PII
S0969805121005047;

Publishing Information

Journal Title
Nuclear Medicine and Biology
Journal Volume
102
Journal Page Range
p. 34-44
ISSN
0969-8051
CODEN
NMBIEO

INIS

Country of Publication
United Kingdom
Country of Input or Organization
International Atomic Energy Agency (IAEA)
INIS RN
53120585
Subject category
S62: RADIOLOGY AND NUCLEAR MEDICINE;
Descriptors DEI
AUTOMATION; AUTORADIOGRAPHY; BIPHENYL; CARBON 11; ESTERIFICATION; ESTERS; EVALUATION; HEART FAILURE; LABELLING; METABOLISM; POSITRON COMPUTED TOMOGRAPHY; RATS
Descriptors DEC
ANIMALS; AROMATICS; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CARBON ISOTOPES; CHEMICAL REACTIONS; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; EMISSION COMPUTED TOMOGRAPHY; EVEN-ODD NUCLEI; HYDROCARBONS; ISOTOPES; LIGHT NUCLEI; MAMMALS; MINUTES LIVING RADIOISOTOPES; NUCLEI; ORGANIC COMPOUNDS; RADIOISOTOPES; RODENTS; SYMPTOMS; TOMOGRAPHY; VERTEBRATES

Optional Information

Copyright
Copyright (c) 2021 Elsevier Inc. All rights reserved.