Test Name Reference Range Acid phosphatase, prostatic, serum 0 – 0.8 U/L ACTH 6.0 – 76.0 pg/mL Alanine aminotransferase (ALT), serum male 10 – 55 U/L female 7 – 30 U/L Albumin, serum 3.5 – 5.2 g/dL Albumin, CSF 11 – 48 mg/dL Aldosterone, serum or plasma Standing (normal salt…
Pharmacology
Compound screening
15. Drug discovery 15.3 Compound screening Peptide deformylase and Met aminopeptidase In vitro screening of Met aminopeptidase inhibitors A non-covalent yet irreversible enzyme inhibitor A generic assay for GPCR activation A cell-based fluorescence assay of membrane depolarization A fluorescence assay of Ca++ influx An in silico docking experiment Electrostatic potential mapped onto the electronic…
Sources of candidate compounds
15. Drug discovery 15.2 Sources of candidate compounds Combinatorial synthesis: the Ugi reaction Semisynthesis of penicillins Semisynthesis of cephalosporins Biosynthesis of polyketides Structure of native 6-deoxyerythronolide B synthase Two compounds produced by engineered variants of 6-deoxyerythronolide B synthase Synthetic libraries Natural compounds Semisynthesis Gene technology Candidate compounds can…
Stages of drug discovery
15. Drug discovery 15.1 Stages of drug discovery Chemical structures of subtype-selective glutamate receptor ligands Target molecule selection validation Candidate compounds acquisition screening Biochemical and physiological discoveries suggest macromolecules that might make worthwhile targets for treating diseases. This is an important step toward new drugs, but only the…
The Viadur® implant
14. Drug delivery 14.7 The Viadur® implant The Viadur® implant is a device for the long-term delivery of leuprolide acetate, an analogue of gonadotropin-releasing hormone (GnRH), the hypothalamic hormone that controls the release of FSH and LH from the anterior pituitary and, through these, of androgens.*…
Delivery of insulin
14. Drug delivery 14.6 Delivery of insulin Aggregation of insulin delays its uptake into the circulation Structure of the insulin hexamer Most body cells require insulin to facilitate uptake of glucose from the blood, and while the plasma insulin level rises and falls in keeping with blood glucose…
Antibodies as drug-targeting devices
14. Drug delivery 14.5 Antibodies as drug-targeting devices Humanized antibodies A calicheamicin-antibody conjugate Activation of calicheamicins DNA cleavage by activated calicheamicins Antibodies have exquisite affinity and selectivity for their targets (antigens) and can be used to direct drugs to specific tissues and cell. In some cases, the antibodies…
Using carriers and vehicles to improve drug delivery
14. Drug delivery 14.4 Using carriers and vehicles to improve drug delivery Protecting drugs from gastric acid through acrylate copolymer coating Site-selective delivery of BCNU Cyclodextrins: Structure and use in drug delivery Solubilization of hydrophobic drugs with surfactants Liposomes as drug delivery vehicles Liposomal vs. deoxycholate-solubilized amphotericin B in a mouse…