Edited by Coastermonger 20:24, September 23, 2010 (UTC)
Describe how histamine is synthesized in vivo.
Histamine is synthesized from Histidine via the enzyme Histidine Decarboxylase (HDC). The molecule is subsequently stored primarily in mast cells.
Recognize the two tautomeric forms of histamine and describe the relevance of these forms.
Describe the different types of histamine receptors.
There are 4 types of histamine receptors. All of them are G protein coupled, they differ in their secondary messengers and tissue distribution.
Receptor Name
Locaion
Action When Stimulated
H1
Smooth Muscle of Intestine
Bronchi
Blood Vessels
Vascular Endothelial Cells
contraction in the ileum
bronchoconstriction
increased capillary permeability (edema)
uticaria (hives) and subsequent of
H2
Gastric Parietal Cells in the stomach
gastric acid secretion
H3
Mainly in the CNS
presynaptic receptors on histamine containing neurons
H4
Describe the mechanism of action of H1 antihistamines.
Describe the structure activity relationship for H1 antihistamines and apply this knowledge to clinical decision making.
Explain the adverse effect profiles of the two generations of H1 antihistamines and describe the differences physicochemically.
Recognize the structures of chromone based mast cell stabilizers.
Describe the mechanism of action of mast cell stabilizers and given a clinical scenario, assess whether a mast cell stabilizer would be appropriate therapy.
Describe the rationale for the design of cimetidine.
Recognize the structures of H2 antagonists.
Describe the mechanism of action of proton pump inhibitors.
Given a structure, predict whether or not the compound would have proton pump inhibition activity.