HT2C Receptors in the Context of Neurotransmitter Receptor Multiplicity 19831988

1.1.1.1 The Concept of Receptor

This chapter is a personal account of how the 5-HT2C receptor was discovered and characterized. The discovery of 5-HT2C receptor took place more than 25 years ago, in the middle of a revolutionary period of change in the receptor concept: the realization that single messengers (such as neurotransmitters) were acting through a multiplicity of receptors. The concept of receptor was initially postulated more than 100 years ago by Paul Ehrlich as "selected binding sites for chemotherapeutic agents" and evolved though the work of J.N. Langley who formulated the concept of "receptive substances" (Bennett 2000).

For many decades, receptors were defined mainly through functional assays based on responses in isolated tissues to chemical series and translated in pharmacological effects in animal models and from there extended to the therapeutic use of such new molecular entities. This concept is the basis for the development of more than 45% of the about 500 known therapeutic targets and for the discovery of numberless drugs.

Despite many decades of receptor research, whether the receptors existed as actual molecular entities was still debated in the 1970s. It was the introduction of radioligand and affinity labeling that led to the solubilization and purification of receptor proteins opening the "molecular era of receptor research" and to the cloning of the first receptors, the cholinergic nicotinic and the b2-adrenergic receptors

BrainCo Biopharma, Parque Tecnol√≥gico de Vizcaya, Edificio 801, 48160 Derio (Bilbao), Spain e-mail: [email protected]

G. Di Giovanni et al. (eds.), 5-HT2C Receptors in the Pathophysiology of CNS Disease, 1

The Receptors 22, DOI 10.1007/978-1-60761-941-3_1, © Springer Science + Business Media, LLC 2011

representing the two big families of receptors, i.e., ligand gated channels and GPCRs (Lefkowitz 2004).

The development of the identification of receptors in cell-free preparations using radiolabeled ligands, a simple tool for the characterization of the recognition sites with the properties of the receptors, in a simple and fast manner, opened new possibilities to study reception. Radioligand binding was expanded later to intact tissue sections for the localization at the light microscope level. These new methodologies revealed many unexpected features of drug and neurotransmitter receptors.

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Defeat Drugs and Live Free

Being addicted to drugs is a complicated matter condition that's been specified as a disorder that evidences in the obsessional thinking about and utilization of drugs. It's a matter that might continue to get worse and become disastrous and deadly if left untreated.

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