Neuroreceptor ligand

The neuroreceptors (ligand-gated ion channels) on the postsynaptic membrane determine the type of synapse ... 

In order to improve the specific activity of [ F]p2 and thus to exploit the electrophilic fluorination also for the production of neuroreceptor ligands, recent studies have addressed the conversion of [ F]fluoride to [ F]F2 with high specific activity, cf.O Fig. 42.9. 

Since it is a benzodiazepine receptor ligand, 11C-flumazenil is primarily used for the neuroreceptor characterization in humans. 

Two classes of membrane residing neuroreceptors can be distinguished a fast ligand-gated channel (class 1) and a slower G protein linked receptor (class 2), which are very similar across a wide range of animals (Table 1). 

Fig. (4). Schematic illustration of ligand-gated ion channels (a nAChR b GABA receptor) and c. G protein linked neuroreceptors.

For this purpose we have determined whether an alkaloid can displace a specifically bound ligand from a neuroreceptor, such as ot, 0t2 adrenergic receptors, serotonin receptor [5-HT2], and nicotinic and muscarinic acetyl choline receptors (Table 15) obtained from porcine brains [69-72]. In addition, we have determined whether the same alkaloids inhibit acetylcholine esterase, whether they intercalate DNA, inhibit DNA polymerase I, reverse transcriptase, protein biosynthesis and membrane stability [40, 73]. The results can be summarized as follows ... 

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