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Index
»
PHARMACOLOGY 1
»
Chapter 2
»
FOUR SUBTYPES OF RECEPTORS
level: FOUR SUBTYPES OF RECEPTORS
Questions and Answers List
level questions: FOUR SUBTYPES OF RECEPTORS
Question
Answer
Ionotropic receptors associated with ligand-gated ion channels Features: LOCATION = __ EFFECT = __
CLASS 1 LOCATION: Cell membrane EFFECT: millisecond
controls Na+ channels (Ligand-gated) -- inhibited by curare and derivatives, ganglionic blockers
Nicotinic Receptor (CLASS 1)
controls Cl- channels
GABAA-receptor complex (CLASS 1)
Metabotropic 7 transmembrane-spanning G-protein-linked Features: LOCATION = __ EFFECT= __
Class II LOCATION: Cell membrane EFFECT: Seconds
G-proteins: __
1) Gs 2) Gi 3) Gq
activates adenylyl cyclase which produces the second messenger cyclic adenosine monophosphate (cAMP)
Gs
inhibits adenylyl cyclase
Gi
activates phospholipase C generating two secondary messengers: 1,4,5- triphosphate (IP3) & diacylglycerol (DAG)
Gq
Enzyme-linked receptors • Features: EFFECT = __; possesses tyrosine kinase activity as part of their structure
Class III EFFECT: minutes to hours
CLASS III example
• Epidermal growth factor • Atrial natriuretic peptide • Insulin
• Intracellular receptors • Features: EFFECT = __
Class IV EFFECT: hours to days
Tubulin is the target of antineoplastic agents such as __
paclitaxel
the total number of cell-surface receptors is reduced, and the cell's responsiveness to ligand is correspondingly diminished because of the rapid degredation those receptors due to accelerated endocytosis
Down Regulation