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Calcitonin gene-related peptide (CGRP) is one of the most potent endogenous vasodilators known. This peptide is increased during migraine attacks and has been implicated in the pathogenesis of migraine headache. Here we report on the ®rst small molecule selective CGRP antagonist: BIBN4096BS. In vitro, this compound is extremely potent at primate CGRP receptors exhibiting an a nity (K i ) for human CGRP receptors of 14.4+6.3 (n=4) pM. In an in vivo model, BIBN4096BS in doses between 1 and 30 mg kg 71 (i.v.) inhibited the e ects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood¯ow in marmoset monkeys. It is concluded that BIBN4096BS is a potent and selective CGRP antagonist.

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A novel method of rare-earth cation-assisted ligand assembly has been developed to provide upconversion nanophosphors with T(1)-enhanced magnetic resonance (MR), radioactivity, and targeted recognition properties, making these nanoparticles potential candidates for multimodal bioimaging. The process of modifying the surface of the nanophosphors has been confirmed by transmission electron microscopy, X-ray powder diffraction, X-ray photoelectron spectroscopy, proton nuclear magnetic resonance, Fourier-transform infrared spectroscopy, energy-dispersive X-ray analysis, and so on. The versatility of this surface modification approach for incorporating functional molecules and fabricating fluorine-18-labeled magnetic-upconversion nanophosphors as multimodal bioprobes has been demonstrated by targeted cell imaging, in vivo upconversion luminescence, MR imaging, and positron emission tomography imaging of whole-body small animals.

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