Development of an 111In-labeled dihydropyridine complex for L-type calcium channel imaging

Preparation and preclinical evaluation of 68Ga-DOTA-amlodipine for L-type calcium channel imaging

“…The toxicity results of the three species including amlodipine itself as the standard are demonstrated in Figure 3 . At almost 1 mg/mL the degree of toxicity is very close for amlodipine and DTPA-AMLO, used in previous studies[ 10 11 ] about 45% cell survival is recorded. However in the case of DOTA-AMLO, at least 35% cell viability is observed showing more toxic effects compared to the other species.…”

“…[ 9 ] Recently, Ga-67 and In-111 DTPA-amlodipine complexes have been reported and were evaluated as possible L-type calcium channel tracers. [ 10 11 ] However, DOTA-conjugates usually offer more radiolabeling opportunities with other diagnostic radionuclides such as Y-86, In-111, Cu-64, and Cu-62, whereas DTPA is mainly applied to In-111 complexes and sometimes lanthanides.…”

L-Type Calcium Channel Blockers: A Potential Novel Therapeutic Approach to Drug Dependence

“…Evidence indicates that the majority of the binding sites in the brain are on neurons rather than blood vessels (Ricci et al, 2002), with the highest concentrations in hippocampus, amygdala, and substantia nigra and the lowest incidence in the cerebellum and brain stem (Cortes et al, 1984). A recent report that L-channels can now be radiolabeled in vivo in rodents (Firouzyar et al, 2015) may open the way for further investigations. Studies have identified the genes encoding of the a1 subunits of the Ca v 1.1 (CACNA1S), Ca v 1.2 (CACNA1C), and Ca v 1.3 (CACNA1D) channels (see Table 1), and alterations in these have been implicated in psychiatric disorders (Heyes et al, 2015).…”