Receptor concept, Ehrlich

Today, it is accepted that Langley and Ehrlich deserve comparable recognition for the introduction of the receptor concept. In the same years, biochemists studying the relationship between substrate concentration and enzyme velocity had also come to think that enzyme molecules must possess an active site that discriminates among various substrates and inhibitors. As often happens, different strands of evidence had converged to point to a single conclusion. 

Ehrlich studied first antimiobial agent, salvarsan, Ksulting fnm systematic synthesis efforts gave rise to receptor concept and chemotherapy concept... 

As for giving a symbolic landmark to drugs history at the beginning of the century, Paul Ehrlich (Institut fiir experi-mentelle Therapie, Frankfurt) (Figure 1.39) introduced, in 1900, the term receptor. The receptor concept as such, was in fact developed in the context of immunology. The drug receptor theory, in turn, would be later developed in Ehrlich s chemotherapy. 

Pharmacophore A pharmacophore is the spatial mutual orientation of atoms or groups of atoms assumed to be recognized by and interact with a receptor or the active site of a receptor. In conjunction with the receptor concept, the notion of a pharmacophore relates directly to the lock-and-key theory proposed by E. Fischer and P. Ehrlich around the beginning of the 20th century (Corpora non agunt nisi fixata). 

The receptor concept was formulated by Langley and the term receptor was proposed by Ehrlich. The concept of receptor binding. Corpora non agunt nisi fixata (compounds do not act unless bound), has been subject to refinement but is still valid. 

Some chemicals, such as strong aids and bases, exert their toxic action in a nonspecific way simply by denaturing protein and dissolving the tissue. Such lesions are referred to as chemical bums. In most cases, however, toxins act by interacting with specific components of the tissue, thus perturbing normal metabolism. Early in the twentieth century Paul Ehrlich proposed the concept of specific receptors (Ehrlich, 1913). He postulated that a chemical, in order to exert biological action, must reach a specific target area and fit into a receptor site. 

The recognition by Paul Ehrlich in 1906 that molecules do not act if they do not bind, Corpora non aguntnisi 6xata in this way Erlich introduced the concept of a biological receptor. 

The concept of receptors is credited to the independent work of Paul Ehrlich (1845-1915) and J. N. Langley (1852-1926). With Ehrlich, the concept appeared to originate from his immunochemical studies on antibody-antigen interactions. Based on the high degree of specificity of antibodies for antigens, Ehrlich postulated the existence of stereospecific, complementary sites on the two molecules. Similar... 

The pharmacological concept of receptors, based upon the observation of rigid structure-activity relationships, stereospecificity, and the observation of maximal pharmacological responses goes back to the turn of the century. More than a hundred years ago, Fischer [1] proposed the lock-and-key model for the enzyme-glycoside system. Later, Langley [2] and Ehrlich [3] further developed this model which can be applied to receptors as well. 

The definition of receptors as specific sites for drug action owes much to the work of John Newton Langley [ 1852-1925 ] and Paul Ehrlich [ 1854-1915 ]. Their separate work on the autonomic nervous system and toxins and chemotherapeutic agents led to the concept of a receptor that possesses both recognition and transduction components and of chemotherapeutic molecules possessing discrete molecular features subserving specific functions ... 

---