Pharmacology 2 Flashcards
Name 2 types of receptors
Nicotinic receptors
Muscarinic receptors
Where are nicotinic receptor?
Found in skeletal muscle ganglia CNS
What is the nicotinic receptor structure?
pentameric structure many subunits combinations
Ligand gated Na+ channel
Where are muscarinic receptors ?
Found in intestinal smooth muscle heart blood vessels salivary glands CNS
How many known subtypes to the muscarinic receptor
5
What are muscarinic receptors coupled with?
G-protein
What activates and blocks Nicotinic receptors?
Activated by nicotine
Blocked by d-tubocurarine
What activates and blocks Muscarinic receptors?
Activated muscarine
Blocked by atropine
What are the subunits in adult muscle nicotinic receptors?
2x Alpha
beta
gama
delta
How many types of Alpha and Beta subunits are there on nicotinic receptors?
8 Alpha
4 Beta
Name the Nicotinic receptor antagonist NMJ
Decamethonium
Name the Nicotinic receptor antagonist at ganglia
Hexamethonium
Name the substance that blocks at NMJ but not a neuronal receptors
Alpha-bungaratoxin
What is epibatidine?
Selective antagonist of neuronal nicotinic receptor
How does having an R group of C2H5 affect the potency and classification of the molecules?
R1 = C2H5 - 25% potency partial agonist R1 = R2 = C2H5 0.03% potency partial agonist R1 = R2 = R3 = C2H5 no agonist activity, weak antagonist
What 4 structural factors affect drug ability
Charge
Methyl Group
Ester linkages
Distance
On a nicotinic receptor what does addition of alpha-methyl mean?
Retains activity
R-isomer 4% activity
S=isomer 1%
On a nicotinic receptor what does addition of beta-methyl mean?
Nicotinic inactive
S-isomer fully active
R isomer 1% active
What are the 3 types of Histamine receptor subtypes
H1- produces vasodilation
H2- stimulates gastric acid secretion
H3- presynaptic receptor
Name an example of an inhibitory amino acid transmitters
GABA
Muscimol
Baclofen
Name an example of an excitatory amino acid transmitter
Glutamate
Aspartate
Name 3 excitatory amino acid transmitters receptors that are ionotropic receptors
NMDA
Kainate
AMPA
AP4 receptor is a m_____ receptor causing increased c____ and release of c____
AP4 receptor is a metabotropic receptor causing increased cAMP and release of Ca2+
GABA is the m___ i____ neurotransmitter in the CNS
major inhibitory neurotransmitter