Tissue Distribution of Intravenously Administrated Poly-Arginine Peptide R18D in Healthy Male Sprague–Dawley Rats

Abstract

Aim: R18D is a poly-arginine peptide that has demonstrated neuroprotection in preclinical models of excitotoxicity, stroke, hypoxic-ischemic encephalopathy and traumatic brain injury. Here, we examined the peptide’s uptake in serum. Materials & methods: Healthy, male Sprague–Dawley rats were intravenously administered either 1000 nmol/kg R18D (D-enantiomer of R18) or approximately 2.5 nmol/kg (36 ± 9 MBq) [18F]R18D, for serum and organ tissue uptake, respectively. Serum samples underwent mass spectrometric analysis to detect unbound R18D peptide. Animals administered [18F]R18D were subjected to positron emission tomography imaging. Results & conclusion: Free R18D was detected at 5 min post-infusion in serum samples. [18F]R18D was rapidly distributed to the kidney (6–7%ID/g), and a small fraction localized to the brain (0.115–0.123%ID/g) over a 60-min acquisition period.