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31 Cards in this Set

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  • Back
What's the main difference in effects between ligand receptors and g protein coupled receptors?
Ligand have rapid, short-acting responses while g protein has slow potentials with long-term effects.
What causes excitatory depolarization (ion-wise)?
More Na+ in or less K+ out
What causes inhibitory hyperpolarization (ion-wise)?
More K+out, more Cl- in or less Na+ in
What are the 4 criteria for being a neurotransmitter?
1. Presence (in the presynaptic terminal)
2. Release (in response to depol, Ca2+ dependent)
3. Identity of action (direct application effects = presynap stim)
4. Removal (1+ mechanisms for elimination)
What synapses are cholinergic?
Neuromuscular, autonomic ganglia, parasymp postgang neuroeffector, sweat glands, between symp pregang and adrenal chromaffin cells, and certain CNS.
What synapses involve norepi (noradrenergic)?
Postgang sympathetics and certain CNS.
What synapses involve epinepherine?
Certain CNS.
Also a hormone released from chromaffin cells.
What synapses involve dopamine?
(dopaminergic)
Postgan sympathetics in the kidney and certain CNS.
Where is nonadrenergic noncholinergic transmission typically found?
Enteric nervous system
What types of transmitters are involved in nonadrenergic noncholinergic transmission and cotransmission?
adenosine 5’-triphosphate (ATP)
vasoactive intestinal peptide (VIP)
neuropeptide Y (NPY)
leutinizing hormone releasing hormone (LHRH)
5-hydroxy tryptamine (5-HT or serotonin)
nitric oxide (NO)
gamma-amino butyric acid (GABA)
substance P
dopamine
Structure of muscarine?
Structure of atropine?
Structure of dopamine?
What's cool about NO?
Cotransmitter at inhib ENS and neuromuscular junctions (especially important at sphincters). Synthesized by NO Synthase when stimulated by Ca2+, can cross membrane without vesicles.
How's ACh made? What's the rate-limiting step?
Synthesized by choline acetyl-transferase in cytosol from acetylCoA and choline. Rate limiting step = choline uptake from ECM via high affinity transporters.
How is ACh broken down?
By Acetylcholinesterase in the synaptic cleft
What compound blocks choline uptake? (synthesis)
Hemicolinium
What compound inhibits the vesicular ACh transporter? (storage)
Vesamicol
What compound blocks exocytosis of ACh by modifying docking proteins and preventing synaptic vesicle fusion with the presynapatic nerve terminal? (release)
Botulinum Toxin
What compound is a nicotinic agonist?
Nicotine (used in Alzheimer's tx)
What compound is a muscarinic agonist?
Bethanacol
What compound is a neuronal nicotinic antagonist?
Trimethaphan (blocks ganglionic transmission - major effect = vasodilation)
What compound is a muscular nicotinic antagonist?
d-tubocurarine (paralyzes somatic muscle)
What compound is a muscarinic antagonist?
Atropine (used locally to dilate the eye and systemically to increase HR and cardiac output)
What compound inhibits acetycholinesterase? (disposition)
physostigmine (used to tx myasthenia graves and glacoma)
In the synthesis of norepi, what is tyrosine converted to? What is the enzyme involved?
Tyrosine is converted to DOPA via Tyrosine Hydroxylase in the cytosol (*rate-limiting step*)
In the synthesis of norepi, what's DOPA converted to? What's the enzyme involved?
DOPA's converted to Dopamime via DOPA decarboxylase in the cytosol
What's dopamine converted to? What's the enzyme involved?
Dopamine's converted to norepi via Dopamine Beta-hydroxylase in the vesicle (*released into cleft when the neurotransmitter is*)
What's alpha2 receptor's major function?
Located at the presynaptic terminal, provides negative feedback to the presynaptic neuron to stop the release of neurotransmitter.
Which of the beta receptors has the highest affinity for norepi?
Beta1
What enzymes metabolize epi and norepi? What are they metabolized into?
MAO and COMT metabolize them to vanillylmandelic acid. (dopamine's metabolized to homovanillic acid)