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23 Cards in this Set
- Front
- Back
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Hemicholiniums
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inhibit choline transporter
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acetylcholine synthesis
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synthesized from choline and acetyl-CoA
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choline acetyltransferase (ChAT)
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enzyme responsible for acetlycholine synthesis
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Vesicle-associated transporter (VAT)
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responsible for storing ACh
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Vesamicol
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inhibits vesicle-associated transporter (VAT)
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VAMPs and SNAPs
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Helps ACh storage vesicles associate with the nerve terminal facing the synapse associate with the membrane and release contents into the synaptic cleft
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Botulinum toxin
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removes two AAs from one or more of the fusion proteins (VAMPs and SNAPs) inhibits ACh release
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acetylcholineesterase
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splits acetylcholine into choline and acetate
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Neostigmine
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blocks acetylcholinesterase which enhances acetylcholine effects
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Curare
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Inhibition of nicotinic receptors of both autonomic ganglia and the Motor end plate
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Hexamethonium
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blocks the nictotinic receptor in the ganglie but not on the motor end plate
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Nicotinic receptors
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Are found in hte adrenal medulla, autonomic ganglia, and neuromuscular junction
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rate limiting step in catecholamine synthesis
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conversion of tyrosine to dopa
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metyrosine
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inhibition of tyrosine to dopa
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catechol-O-methyl transferase (COMT)
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metabolizes catecholamines that are in circulation through simple diffusion
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Norepinephrine transporter (NET)
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reuptakes NE back into the synaptic cleft
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Cocaine and tricyclic antidepressant drugs
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intibit the reuptake of NET which increases NE activity in the synaptic cleft
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Extraneuronal transporters (ENT/NET2)
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take up catecholamines
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corticosteroids
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inhibit reuptake of catecholamines by inhibition of ENT/NET2
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monoamine oxidase (MAO)
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metabloizes reuptaken catecholamines, a mitochondrial enzyme
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Tyramine
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release may cause hypertensive crisis caused by irreversible antagonists of MAO
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Reserpine
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inhibits the storage of catecholamines which are transported by vesicular monoamine transporter (VMAT)
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Bretylium
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inhibits VAMP which helps with vesicle fusion of NE on the snaptic cleft
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