Drug Discrimination: Applications to Medicinal Chemistry and Drug Studies

Drug Discrimination: Applications to Medicinal Chemistry and Drug Studies

Language: English

Pages: 530

ISBN: 0470433523

Format: PDF / Kindle (mobi) / ePub


Drug discrimination: a practical guide to its contributions to the invention of new chemical entities and evaluations of new or known pharmacological agents

Drug discrimination can be described as a "drug detection" procedure that uses a pharmacologically active agent as the subjective stimulus. Although the procedure does require some effort to implement, it can be an extremely important tool for understanding drug action. Whereas medicinal chemists should come to learn the types of information that drug discrimination studies can offer, pharmacologists and psychologists might come to realize how medicinal chemists can apply the types of information that the paradigm routinely provides. Drug Discrimination: Applications to Medicinal Chemistry and Drug Studies provides in-depth analyses of the nature and use of drugs as discriminative stimuli and bridges some of the numerous gaps between medicinal chemistry, pharmacology, and psychology.

Stressing the practical aspects of drug discrimination, including types of procedures, study design, data, and interpretation, the book details the advantages and limitations of drug discrimination studies versus other pharmacologic evaluations. Practical information from leading researchers in the field addresses specific topics and techniques that are of interest in drug discovery, evaluation, and development.

A groundbreaking new guide to the applications of drug discrimination studies for medicinal chemistry and neuroscience, Drug Discrimination is essential for any scientist, researcher, or student whose interests involve the design, development, and/or action of drugs acting at the level of the central nervous system.

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discriminate diazepam from vehicle do not recognize morphine. In some instances, administration of a test drug will result in “partial generalization” (≥20%, but ≤80% drug-appropriate responding), which is acknowledged to be the most difficult type of result to interpret; this will be discussed in greater detail later (Chapter 3). Generally, doses of a challenge drug are administered until either stimulus generalization occurs, or until the animal’s behavior is disrupted. In tests of stimulus

characteristics. As can be seen, most of the studies reported that different doses of the same drug can produce, to some degree, dissimilar stimulus effects. For example, rats trained to discriminate the effects of 0.3 mg/kg, but not 10 mg/kg, of morphine generalized c03.indd 71 6/7/2011 7:11:21 PM 72 DRUG DISCRIMINATION: PRACTICAL CONSIDERATIONS TABLE 3-6. List of studies that employed separate groups of subjects trained to discriminate different doses of the same drug from vehicle and

such as nitro- or carbonyl-reductions and dehalogenation (e.g., halothane). Phase II reactions, usually known as conjugation reactions [e.g., with glucuronic acid, sulfonates (usually referred to as sulfation), glutathione, or amino acids], typically involve the attachment of a more polar molecule (i.e., hydrophilic group) to the original drug molecule to increase water solubility, thereby permitting more rapid drug excretion. Substrates for these reactions include both metabolites of phase I

administration of 2.0 mg/kg to 3.0 mg/kg of S(+)-amphetamine produced disruption of behavior (i.e., no responding; data not depicted). D and S represent percent diazepam-appropriate responding following the training dose of 3.0 mg/kg of diazepam and saline vehicle, respectively. c03.indd 80 6/7/2011 7:11:21 PM DATA ANALYSIS AND INTERPRETATIONS 81 First, lower doses of diazepam were administered to produce a dose response function; subjects responded progressively less on the

Discriminative stimulus properties of toluene in the mouse. Toxicology and Applied Pharmacology, 88, 97–104. 81. Oliveto, A.H., Bickel, W.K., Hughes, J.R., Higgins, S.T., Fenwick, J.W. (1992). Triazolam as a discriminative stimulus in humans. Drug and Alcohol Dependence, 30, 133–142. 82. Karas, C.A., Picker, M.J., Poling, A. (1985). Discriminative stimulus properties of tripelennamine in the pigeon. Psychopharmacology, 86, 356–358. 83. Winter, J.C. (1978). Yohimbine-induced stimulus control in

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