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A stable neurotensin-based radiopharmaceutical for targeted imaging and therapy of neurotensin receptor-positive tumours  

International Nuclear Information System (INIS)

Neurotensin (NT) and its high affinity receptor (NTR1) are involved in several neoplastic processes. Thus, NT-based radiopharmaceuticals are potential tracers for targeted diagnosis and therapy of NTR-positive tumours. A new analogue based on NT(8-13), NT-XIX, with the three enzymatic cleavage sites stabilised, was synthesised and tested. The synthesis was performed by Boc strategy. Labelling with "9"9"mTc/"1"8"8Re was performed using the tricarbonyl technique. Metabolic stability was tested in vitro and in vivo. NT-XIX was further characterised in vitro in HT-29 cells and in vivo in nude mice with HT-29 xenografts. NT-XIX showed much longer half-lives than non-stabilised analogues. Binding to NTR1 was highly specific, although the affinity was lower than that of natural NT. Bound activity rapidly internalised into HT-29 cells and 50% remained trapped after 24 h. In the time-course biodistribution, the highest uptake was ...

2009-01-01

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Stabilization and limit theorems for geometric functionals of Gibbs point processes  

CERN Document Server

Given a Gibbs point process $\\P^{\\Psi}$ on $\\R^d$ having a weak enough potential $\\Psi$, we consider the random measures $\\mu_\\la := \\sum_{x \\in \\P^{\\Psi} \\cap Q_\\la} \\xi(x, \\P^{\\Psi} \\cap Q_\\la) \\delta_{x/\\la^{1/d}}$, where $Q_{\\la} := [-\\la^{1/d}/2,\\la^{1/d}/2]^d$ is the volume $\\la$ cube and where $\\xi(\\cdot,\\cdot)$ is a translation invariant stabilizing functional. Subject to $\\Psi$ satisfying a localization property and translation invariance, we establish weak laws of large numbers for $\\la^{-1} \\mu_\\la(f)$, $f$ a bounded test function on $\\R^d$, and weak convergence of $\\la^{-1/2} \\mu_\\la(f),$ suitably centered, to a Gaussian field acting on bounded test functions. The result yields limit laws for geometric functionals on Gibbs point processes including the Strauss and area interaction point processes as well as more general point processes defined by the Widom-Rowlinson and hard-core model. We provide applications to random ...

2008-01-01