TAILIEUCHUNG - Color Atlas of Pharmacology (Part 7): Drug-Receptor Interaction

Drug-Receptor Interaction partial charges. When a hydrogen atom bearing a partial positive charge bridges two atoms bearing a partial negative charge, a hydrogen bond is created. A van der Waals’ bond (B) is formed between apolar molecular groups that have come into close proximity. Spontaneous transient distortion of electron clouds (momentary faint dipole, !!) may induce an opposite dipole in the neighboring molecule. The van der Waals’ bond, therefore, is a form of electrostatic attraction, albeit of very low strength (inversely proportional to the seventh power of the distance). Hydrophobic interaction (C). The attraction between the dipoles of water is. | 58 Drug-Receptor Interaction Types of Binding Forces Unless a drug comes into contact with intrinsic structures of the body it cannot affect body function. Covalent bond. Two atoms enter a covalent bond if each donates an electron to a shared electron pair cloud . This state is depicted in structural formulas by a dash. The covalent bond is firm that is not reversible or only poorly so. Few drugs are covalently bound to biological structures. The bond and possibly the effect persist for a long time after intake of a drug has been discontinued making therapy difficult to control. Examples include alkylating cytostatics p. 298 or organophosphates p. 102 . Conjugation reactions occurring in biotransformation also represent a covalent linkage . to glucuronic acid p. 38 . Noncovalent bond. There is no formation of a shared electron pair. The bond is reversible and typical of most drug-receptor interactions. Since a drug usually attaches to its site of action by multiple contacts several of the types of bonds described below may participate. Electrostatic attraction A . A positive and negative charge attract each other. lonic interaction An ion is a particle charged either positively cation or negatively anion . the atom lacks or has surplus electrons respectively. Attraction between ions of opposite charge is inversely proportional to the square of the distance between them it is the initial force drawing a charged drug to its binding site. Ionic bonds have a relatively high stability. Dipole-ion interaction When bond electrons are asymmetrically distributed over both atomic nuclei one atom will bear a negative 6- and its partner a positive 6 partial charge. The molecule thus presents a positive and a negative pole . has polarity or a dipole. A partial charge can interact electrostatically with an ion of opposite charge. Dipole-dipole interaction is the electrostatic attraction between opposite partial charges. When a hydrogen atom bearing a partial positive .

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