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At least 19 recordsLinked to original sources
PubMed1983

Gastrointestinal drug receptors.

Drug receptors consist of recognition sites coupled to transducer and cellular amplifier mechanisms. Slight differences in receptor recognition sites can be exploited pharmacologically to provide drugs with a high degree of selectivity for activating or blocking individual receptor subtypes. For example, it may now be possible to block, selectively, subtypes of muscarinic cholinergic receptors in the gastrointestinal tract with pirenzepine and other drugs that discriminate between subtypes of muscarinic cholinergic receptors. The recognition of subtypes of adrenergic receptors may allow highly selective pharmacological activation and blockage of gastrointestinal neural and smooth muscle receptors. The development of nonpeptide receptor antagonists of gastrointestinal hormones and peptide neurotransmitters also offers promise for improved therapy of digestive diseases. Tremendous progress has occurred in recent years in defining multiple types of opioid receptors that alter gastrointestinal secretory, absorptive and motility functions. These receptors are located in the mucosa, nerves and muscle of the intestine and in the brain and spinal cord.

Animals↗
PubMed2005

Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.

Drug-receptor binding thermodynamics has proved to be a valid tool for pharmacological and pharmaceutical characterization of molecular mechanisms of receptor-recognition phenomena. The large number of membrane receptors so far studied has led to the discovery of enthalpy-entropy compensation effects in drug-receptor binding and discrimination between agonists and antagonists by thermodynamic methods. Since a single thermodynamic study on cytoplasmic receptors was known, this paper reports on binding thermodynamics of estradiol, ORG2058, and R1881 bound to estrogen, progesterone, and androgen steroid/nuclear receptors, respectively, as determined by variable-temperature binding constant measurements. The binding at 25 degrees C appears enthalpy/entropy-driven (-53.0 </= DeltaG degrees </= -48.6, -34.5 </= DeltaH degrees </= -19.9 kJ/mol, 0.057 </= DeltaS degrees </= 0.111, and -2.4 </= DeltaC(p) degrees </= -1.7 kJ mol(-1) K(-1)) and is interpreted in terms of hydrophobic and hydrogen-bonded specific interactions. Results obtained for cytoplasmic receptors are extensively compared with those known for typical membrane receptors, in particular the adenosine A(1) receptor, to investigate the thermodynamic bases of drug-receptor binding from the most general point of view.

Estradiol↗
PubMed2003

Receptor-drug association studies in the inhibition of the hematin aggregation process of malaria.

Docking studies were performed to investigate the binding of several antimalarial compounds to the putative drug receptors involved in the hematin aggregation process. These studies reveal a binding profile that correlates with the complementarity of electrostatic potentials between the receptors and the active molecules. These results allow a possible explanation for the same molecular mechanism shown by 4-aminoquinolines, quinine, mefloquine, halofantrine and hydroxylated xanthones. The docking data presented in this work offer an interesting approach to the design of new molecules with potential antimalarial activity.

Antimalarials↗
PubMed1982

The use of drug-receptor affinity measures in the differentiation of receptors.

The drug-receptor dissociation constant (K), determined by pharmacological procedures, is measured from a dose-effect relation and the modification of that relation by the presence of a second compound (antagonist) that competes for the same receptor. These procedures differ from those that use radiolabeled compounds and do not measure an effect but instead determine the K of the compound by quantitating its displacement of the labeled substance. In several examples the dissociation constants determined from pharmacological procedures are shown to be unique for a particular drug-receptor interaction and can therefore discriminate among receptors. A further demonstration is that K does not equal D50, the potency index. For competitive antagonists the Schild plot is commonly used to measure K. This plot, theoretically linear with a slope of -1, often leads to slopes different from -1 (using conventional linear regression), in which case its x intercept, pA2, and y intercept, -log KB, differ by an amount that depends on the slope. Even when this differences is small, the 95% confidence limits of pA2 and -log KB may be very different and are invariably larger for -log KB, the value that is presumably sought from this analysis. A Schild plot constrained to slope -1 (and, accordingly, different regression equations) should therefore be used in cases of known competitive antagonism such as that between naloxone and morphine. The special problems associated with measuring K for agonists are discussed and illustrated with recent work done in our laboratories in which we employed the new narcotic analgesic buprenorphine to determine by pharmacological methods the dissociation constant for morphine, a value previously undetermined.

Adrenergic alpha-Agonists↗
PubMed1989

Challenges for receptor theory as a tool for drug and drug receptor classification.

Increased understanding in the field of receptor pharmacology, born of the sophisticated techniques now available to us, has confounded rather than simplified the problem of receptor classification. The International Union of Pharmacology (IUPHAR) is currently sponsoring a Receptor Nomenclature Committee whose aims are to recommend a rational system of classification, a formidable task given the complexity and volume of data in the literature (agonist/antagonist potencies, coupling mechanisms, primary structures, etc.) that will need to be incorporated. The Committee's chairman, Terry Kenakin, outlines here the limitations of classical receptor theory for drug receptor classification and suggests that any functional classification system must take into account not only affinity and intrinsic efficacy but also, at the very least, parameters relating to the transducing properties of receptors. If this is not done, then receptor classification data obtained from studies with agonists and antagonists may be different and lead to confusion.

Animals↗
PubMed1978

Methodological aspects on drug receptor binding analysis.

Although drug receptors occur in relatively low concentrations, they can be visualized by the use of appropriate radioindicators. In most cases the procedure is rapid and can reach a high degree of accuracy. Specificity of the interaction is studied by competition analysis. The necessity of using several radioindicators to define a receptor population is emphasized. It may be possible to define isorecptors and drugs with selectivity for one isoreceptor.

Animals↗