Studies of multiple morphine and enkephalin receptors: evidence for mu1 receptors.
Studies of multiple morphine and enkephalin receptors: evidence for mu1 receptors.
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DOI：
10.1007/978-1-4757-5971-6_7
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发表时间：
1988
影响因子：
--
通讯作者：
G. Pasternak
中科院分区：
文献类型：
--
作者：
G. Pasternak
The concept of receptors plays in integral role in pharmacology. Many drugs act through interactions with specific binding sites and dissociate unchanged, unlike enzymes which modify subtrates. The realization that subtypes of receptors for a ligand may exist has opened a number of possibilities in drug development and remains important. In the past, the classification of receptor subtypes rested heavily upon either classical bioassays or in vivo studies. More recently, the availability of binding assays has permitted a more molecular approach to this question. Both approaches have their advantages and disadvantages. These are important issues since the development of highly selective drugs is often based upon the identification of subtypes of receptors with highly selective functions.Binding assays offer a direct assessment of the affinity of specific ligands to the binding site. Comparing the interactions of various drugs, one can assess the presence of multiple classes of sites. Scatchard analysis of saturation experiments and detailed competition studies, coupled with sophisticated computer analysis programs, such as LIGAND (Munson and Rodbard, 1980) can provide evidence for multiplicity of sites varying either in affinity for a ligand or by selectivity among different compounds. However, this type of analysis is heavily dependent upon the assumptions upon which the computer programs are based. Interpreting the results of these binding assays can be difficult. For example, evidence for two sites with differing affinities for a ligand might represent separate classes of receptors or just conformational differences for a single one. Furthermore, a" novel" binding site might truely be unique or may simply represents cross-binding to a site for a different class of ligand.
