Receptors I

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Marge1  on January 21, 2012

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Receptors I

cholinergic receptors divided intwo what two categories?
nicotinic and muscarinic
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cholinergic receptors divided intwo what two categories? nicotinic and muscarinic
Nicotinic Nn receptor location: postganglioanic neurons and CNS.
result of activation: opeining of Na and K channels, depolarization.
Nicotinic Nm receptor location: skeletal muscle (neuromuscular junction)
result of activation: opening of Na and K channels, depolarization
receptor channels are compoed of how many subunits? 5
what distingueses Nn from Nm the differences in the subunit proteins.
Receptor channels; each subunit has.. 4 different channels hat cross the plasma membrane to make the pore.
pore of receptor channels lined by? M2 unit. (formed by M2 segment from each of the protein subunits.)
Pore of receptor channels shape? narrow in middle. selective for size and charge. (negatively charged at openings).
In order for receptor channel to open, it requires? two molecules of Ach to bind on the alpha subunit. (causes equilibrium state betwen open state and closed state.)
Neostigmine: cholinesterase inhibitor added to virtual cat HR: decreases. Why? blocks acetylcholinesterase. Ach present longer.
Acts at SA node at M2 receptor.
BP: decreases due to HR change
muscle: increased contraction (ach there longer)
adrenergic receptor: alpha 1 tissue: vascular smooth muscle
effect: constricsts smooth muscle, increases BP
adrenergic receptor: alpha 2 tissue/ex: auto-receptor
effect: decreases neurotransmitter release
adrenergic receptor: beta 1 tissue: heart
effect: increase HR and heart force
adrenergic receptor: beta 2 tissue: smooth muscle (bronchial)
effect: relaxation of smooth muscle
adrenergic receptor: beta 3 tissue: adipose
effect:stimulate breakdown of lipids (active in fight or flight)
All muscarinic and adrenergic receptors are? G protein coupled receptors
N terminous end of G protein coupled receptor is where? extracellular
where is C terminous end of G protein coupled receptor? intracellular
Approx. how many G protein coupled receptors are there? over 1,000
G protein coupled receptors are the largest target for? drugs
Inactive G protein alpha subunit bound to GDP. beta and gamma subunits boud to alpha. entire complex is together.
what is roll of G protein coupled receptor? promote exchange from GTP to GDP
Once alpha subunit sees an available GTP, it will? bind the GTP and kick off a GDP.
After alpha subunit binds the GTP what happens? the beta and gamma stay together and the alpha dissociates from them and alpha subunit has intrinsic GTPase activity
what is alpha subunit's intrinsic GTPase activity? takes off phosphate leaving GDP. The GDP and alpha then associate with the beta and gamma subunits. this turns off the system. cycle begins again.
Gi and Gs tend to work against each other, but have? overlapping effects.
Gs-stimulatory
Gi-inhibitory
Go receptor? inhibits voltage-gated Ca2+ channels
very similar/overlaps with Gi
Gq receptor activates pospholpase C
G 12/13 receptor promotes growth and differentiation

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