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28 Cards in this Set
- Front
- Back
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1. What is precursor of glutamate? 2. What is the precursor of GABA? |
1. Glutamine 2. Glutamate |
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What is the function of VGLUT 1 & 2?
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VGLUT = vesicular glutamate transporter packages glutamate into vesicles; these vesicles will release their glutamate content into the synapse. release into synapse is Calcium dependent |
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How is glutamate removed from the synaptic cleft? |
EAAT = excitatory amino acid transporter |
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What are the two glutamate receptor families? |
1. Ionotropic: fast signaling = excitatory post synaptic response -Kainate = influx of Na -NMDA influx of Na and Ca -AMPA = influx of NA 2. Metabotropic: slower, G-protein second messenger system |
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Describe the NMDA receptor. |
requires both glutamate and glycine (glycine is the co-agonist) in order to open the ion channel
-resting potential: Mg ion inside channel, which blocks it; depolarization has to occur to dissociate Mg from receptor
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What antagonists bind at a 2nd binding site within the NMDA receptor channel to block it? |
phencyclidine and ketamine |
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From a clinical standpoint, high levels of glutamate are ________________ to neurons. |
excitotoxic |
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Describe the clinical aspect of Ischemia relating to glutamate. |
When ischemia occurs, there is massive release of glutamate in the affected area. This results in prolonged activation of NMDA receptors.
personal side note :) prolonged NMDA receptor activation results in massive Ca influx into neuron = activation of enzymes (like endonucleases, phospholipases) that damage the cell |
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What type of drugs may assist in reducing focal ischemic adverse effects? |
NMDA antagonists glycine site antagonists |
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ALS stems from a defect in ______________. What drug is used to assist in treating the problem associated with this defect? |
EAAT2 -- which means, cannot have effective reuptake of glutamate Riluzole blocks NMDA receptors |
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1. What is the function of VGAT? 2. What is the function of GAT? 3. What function of GABA-T? |
1. Vesicular GABA transporter = transports GABA into synaptic vesicles 2. GABA transporter = removes GABA from synaptic cleft 3. GABA aminotransferase = within the neuron during recycling, it metabolizes GABA to glutamate |
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Which is ionotropic vs. metabotropic? GABAA and GABAB? |
GABAA = ionotropic (more prevelant) GABAB = metabotropic |
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Describe the GABAA receptor and function. |
heteropentameric complex = combination of 5 subunits will cause Cl influx to result in hyperpolarization of neuron = inhibitory |
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What are the positive allosteric modulators of the GABAA receptor? |
anxiolytic, sedative-hypnotic, antispastic, anticonvulsant and can induce anesthesia |
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What are the negative allosteric modulators of the GABAA receptor? |
proconvulsant, anxiogenic, memory enhancing |
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1. ________________increase duration of the GABAA receptor ion channel opening. 2. ________________increase frequency of GABAA receptor ion channel opening. |
1. Barbs 2. Benzos |
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Tiagabine MOA and use ? |
inhibits GAT-1 = increase in extracellular GABA partial seizures |
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Vigabatrin MOA and use? |
inhibits GABA-T = prevents GABA metabolism (breakdown) infantile spasms and adjunctive therapy for adults with refractory complex partial seizures |
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List the 2 GABAB agonists and their use. |
Baclofen = muscle relaxant/antispasmodic GHB = narcolepsy |
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What is the function of VMAT? |
Vesicular monoamine transporter = transports 5-HT into synaptic vesicles |
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What is the function of auto-receptors found on the cell body, dendrites and terminals of 5-HT neurons? |
binding to this receptor site will result in inhibition of 5-HT from neuron |
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What is the function of the 5-HT transporter? |
5-HT is rapidly removed from synaptic cleft by this reuptake transporter |
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Antipsychotics generally block what type of receptor? |
5-HT-2a increase serotonin is associated with psychosis (schizophrenia) antagonists include: ritanserin risperidone clozapine |
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What is the result of an agonist to the 5-HT-1a receptor? Name drug involved in this mechanism. |
5-HT-1a is a auto receptor. IF an agonist binds to this receptor, it will result in: --reduced appetite = weight loss --reduced anxiety (buspirone) |
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What is the result of an agonist to the 5-HT-1D/1B receptor? Name drugs involved in this mechanism. |
agonists: treatment of migraine headaches also, reduces trigeminal pain pathway "--triptans" (i.e. sumatriptan) |
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What is the result of blocking 5-HT-3 receptor? Name drugs involved in this mechanism. |
prevent nausea and vomiting due to surgery/chemotherapy -setron (i.e. ondanestron) |
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1. Where are CB1 receptors located and what are they responsible for? 2. What are the 2 primary endogenous cannabinoids that bind to this receptor?
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1. CNS and responsible for psychoactive effects 2. anandamide and 2-arachidonylglycerol (2-AG) |
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MOA of endocannabinoid receptor activation? |
exhibit retrograde synaptic signaling to inhibit GABA involved in memory, appetite, pain, immunomodulation, analgesia |
