| Drugs acting on adrenergic neurotransmission: | Alpha-Methyltyrosine: inhibits norepinephrine synthesis; cocaine: inhibits norepinephrine reuptake; amphetamine: enhances norepinephrine release |
| Examples of drugs that act on ion pumps and transporters in nephron epithelial cells: | Amiloride, chlorothiazide, furosemide and related agents |
| An example of an agent which changes ion pump expression in nephron epithelial cells: | Aldosterone |
| Examples of functional domains associated with drug receptors: | An effector domain and a ligand-binding domain (here the ligand may be a drug or hormone, for example) |
| An example of a drug which targets an extracellular ligand-binding receptor domain: | Propranolol, prazosin and other ß-adrenergic antagonists-there are many other examples. |
| A monoclonal antibody targeting The extracellular binding domain of epidermal growth factor in inhibits epidermal growth factor signaling: | Cetuximab (Erbitux) |
| Examples of small molecule drugs binding to the intracellular effector domain and blocking protein tyrosine kinase activity of activated epidermal growth factor receptor: | Gefitinib (Iressa) and erlotinib (Tarceva) |
| Example of scaffolding or anchoring proteins which localize signaling pathways by protein--protein interactions: | A-kinase anchoring proteins (AKAPs)-These protein molecules bind the regulatory subunit of cyclic AMP dependent protein kinase near its substrate. |
| Effect on cardiac myocytes as a result of increased cellular cyclic AMP due to activation of ß-adrenergic receptors: | Increased cardiac contractility by enhancing the rate and amount of calcium available to the contractile system. |
| Effect of cyclic GMP and calcium ions on smooth muscle cell contractility: | Relaxation-as a result of activation of the cyclic GMP-protein kinase pathway which phosphorylates proteins that mediate calcium signaling including myosin light chain kinase and ion channels leading to cell membrane hyperpolarization. |
| Some characteristics of G protein-coupled receptors (GCPRS): | Characterized by seven transmembrane alpha helices; third-largest human gene family; associated with numerous physiological activities including smell, vision, taste, nerve activity, metabolism, smooth muscle tension, cardiac contractility, and glandular secretion. |
| Ligands for G protein-coupled receptors include: | Opioids, norepinephrine, acetylcholine, eicosanoids, peptide hormones, GABA. |
| G protein-coupled receptors (GPCRs) couple to this family: | The family of heterotrimeric GTP-binding regulatory proteins (G proteins) |
| G protein heterotrimers include: | A guanine nucleotide alpha subunit, and associated dimers consisting of ß and gamma subunits. |
| These G protein dimers facilitate membrane localization of the G protein heterotrimer: | ß and gamma subunits |
| This G protein constituent is involved in recognition of both receptors and effector molecules: | The alpha subunit |
| The Gs alpha protein subunit exhibits this effect on adenylyl cyclase: | Activation of the enzyme |
| The Gi alpha subunit is likely to have this effect on certain adenylyl cyclase isoforms: | Inhibition of certain isoforms of adenylyl cyclase |
| The Gq alpha subunit exhibits this effect on phospholipase C ß: | activation of all forms of phospholipase Cß |
| Notable action of G12/13 alpha subunits: | Coupling to guanine nucleotide exchange factors (GEFs) |