Pharmacodynamics I

Question 1

local anesthetics block _____ in neurons that transmit pain information from the periphery to the CNS

Answer 1

local anesthetics block voltage-gated sodium channels in neurons that transmit pain information from the periphery to the CNS

Question 2

benzodiazepines bind to the GABA_A receptor in neuronal membranes in the CNS

Answer 2

benzodiazepines bind to the ____ receptor in neuronal membranes in the CNS

Question 3

binding of benzodiazepines to the receptor enhances the ability of ____ to open the chloride channel, thereby hyperpolarizing the neuron

Answer 3

binding of benzodiazepines to the receptor enhances the ability of GABA to open the chloride channel, thereby hyperpolarizing the neuron

Question 4

binding of benzodiazepines to the receptor enhances the ability of GABA to open the _____, thereby hyperpolarizing the neuron

Answer 4

binding of benzodiazepines to the receptor enhances the ability of GABA to open the chloride channel, thereby hyperpolarizing the neuron

Question 5

binding of benzodiazepines to the receptor enhances the ability of GABA to open the chloride channel, thereby ____ the neuron

Answer 5

binding of benzodiazepines to the receptor enhances the ability of GABA to open the chloride channel, thereby hyperpolarizing the neuron

Question 6

what are the 3 components to a G protein-linked receptor?

Answer 6

• a cell-surface receptor
• a G protein
• an effector: an enzyme or an ion channel

Question 7

in the unstimulated state, the α subunit has ____ bound; when a hormone binds to a G protein-linked receptor, the receptor undergoes conformational change that exchanges the ___ for ___

Answer 7

in the unstimulated state, the α subunit has GDP bound; when a hormone binds to a G protein-linked receptor, the receptor undergoes conformational change that exchanges the GDP for GTP

Question 8

the in the unstimulated state, the α subunit also has ____ activity; after some time, it hydrolyzes ___ to ___, and the α subunit reassociates with the ___ complex

Answer 8

the in the unstimulated state, the α subunit also has GTPase activity; after some time, it hydrolyzes GTP to GDP, and the α subunit reassociates with the βγ complex

Question 9

phospholipase C hydrolizes PIP2 into ___ and ___; ___triggers release of Ca2+ from the ER

Answer 9

phospholipase C hydrolizes PIP2 into DAG and IP3; IP3 triggers release of Ca2+ from the ER

Question 10

what are the 2 types of enzyme-linked receptors?

Answer 10

• ligand-regulated transmembrane enzymes
• cytokine receptors

Question 11

the largest group of transmembrane receptors with enzymatic cytosolic domains is the ____ family

this class of receptors includes which 4 receptors?

Answer 11

the largest group of transmembrane receptors with enzymatic cytosolic domains is the receptor tyrosine kinase family

this class of receptors includes:

• insulin receptor
• epidermal growth factor receptor (EGFR)
• platelet-derived growth factor (PDGFR)
• nerve growth factor receptor (NGFR)

Question 12

_____ mutations in tyrosine kinase receptors can lead to cancer

Answer 12

gain-of-function mutations in tyrosine kinase receptors can lead to cancer

Question 13

____ use a mechanism resembling that of receptor tyrosine kinases, except that in this case, the protein tyrosine kinase activity is not intrinsic to the receptor molecule; instead the intracellular domain of the receptor binds an ____ from the ____family

Answer 13

cytokine receptors use a mechanism resembling that of receptor tyrosine kinases, except that in this case, the protein tyrosine kinase activity is not intrinsic to the receptor molecule; instead the intracellular domain of the receptor binds an intracellular tyrosine kinase from the JAK family

Question 14

cytokine receptors dimerize upon binding to the activating ligand, leading to activation of the bound ___ which then ____ on the receptor

Answer 14

cytokine receptors dimerize upon binding to the activating ligand, leading to activation of the bound JAKs which then phosphorylate tyrosine residues on the receptor

Question 15

in the cytokine receptor pathway, JAKs also phosphorylate ___, which ____ and translocate to the ____

Answer 15

in the cytokine receptor pathway, JAKs also phosphorylate STATs, which dimerize and translocate to the nucleus to regulate transcription of specific genes