Term
a catechol group is a phenol group with -OH attached in which two positions? |
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Definition
3 and 4.
catechlamines are synthesised from tyrosine and these include noradrenaline, adrenaline and dopamine. the brain lacks phenyalanine hydroxylase. it converts Phe to Tyr thus Tyr is transported into the brain from blood |
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Term
dopamine is associated with motor function and is lost in which disease?
which enzymes are involved in catabolism of catecholamines? |
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Definition
Parkinson's disease.
catabolism involves monoamine oxidase (MAO) and catechol 0-methyltransferase (COMT) |
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Term
Parkinson's was first described in 1817 by J parkinson. the mean age of onset is ~60. it is characterised by 3 main symptoms: muscle rigidity, tremor and bradykinesia. what is bradykinesisa? |
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Definition
slowness of movement.
this is a multifactorial dsease involving age, environmental factors and genetics.
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Term
PD is due to degeneration of pigmented cells of which region in thebasal ganglia? |
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Definition
substantia nigra pars compacta
(shit thats a mouthfull)
as substantia nigra specifially uses dopamine, PD results in >50% depletion of this transmitter |
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Term
why must we use L-dopa and not dopamine itself to alleviate symptom of PD? |
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Definition
because dopamine cannot cross the blood brain barrier but L-dopa can. so it is transported into the brain then turned into dopamine. |
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Term
how is metabolism of L-dopa to dopamine prevented in the periphery? |
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Definition
by a simultaneous admnistration of a Dopa decarboxylase inhibitor which cannot penetrate the blood-brain barrier.
also inhibitors of MAO and COMT can be given to inhibit dopamine degradation.
PD patients are usually given a cocktail of L-dopa, DDI, MAO and COMT |
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Term
serotonin (5-HT) is synthethised from tryptophan by which two enzymes?
how many different types of receptors does it bind to? |
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Definition
tryptophan hydroxylase and 5-hydroxytryptophan (5-HTP) decarboxylase.
14 different types of receptors |
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Term
in ralation to serotonin, what affect do hallucegenic drugs such as LSD have?
the action of serotonin can be terminated mainly by reuptake from the synapse via the 5-HT reuptake transporter on the presynaptic neuron. what else can inactivate the action? |
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Definition
they act as 5-HT agonists and mimick the action of serotonin at 5-HT2A receptors.
serotonin action can also be terminated by MAO. |
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Term
true or false?
amino acids are present at a higher concentration (30mM) than in any other body tissue |
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Definition
true.
these are all non essential amino acids made in situ from glycolytic and citric acid cycle intermediates.
dicarboxylic amino acids glutamate and aspartate are excitatory whereas glycine and GABA are inhibitory
Glutamate and GABA are major transmitters in the brain.
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Term
the most common type of neurotransmitter in the h........ are peptide transmitters. they are synthesised as large precursor p...... then transported to synaptic release site and activated by proteolytic c........ |
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Definition
hypothalamus, proteins, cleavage
peptide transmitters have slow potsynaptic effects and their actions are terminated by extracellular proteases. they are often co-released with other transmitters. includes opioids - endophins, enkephalins and dynorphins
other examples are substance P, neurotensin, vasoactive intestinal peptide (VIP) |
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Term
other transmitters include purines (ATP,GTP and others) Histamine and gases such as Nitric Oxide. NO is not stored in synaptic vesicles as it is a gas but instead is made when required by NOS from arginine. how do NO propagate and terminate? |
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Definition
it diffuses from nerve terminals inot adjacent cells forming covalent linkages to a multiplicity of targets, which maybe enzymes or other targets.
inactivation presumably involves diffusion away. |
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Term
describe the 2 main types of transmitter receptors |
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Definition
ionotropic receptor - fast, few milliseconds and always stimulatory - transmitter acts directly on a ligand gated ion channel to open the channel
metabotropic receptor - slow up to hours, can trigger opening/closing of a seperate ion channel and also other effects on cell - acts indirectly on a GPCR |
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Term
which one is a direct and which is an indirect receptor from nicotinic and muscarinic receptors? |
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Definition
nitotinic is direct
muscarinic is indirect and has five subtypes
M1,M2,M3,M4,& M5 |
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Term
how a G protein acts indirectly on an ion channel. A...... binds to receptor. GTP exchnages for G.... on the a...... subunit. G protein dissociates from receptor with its 3 subunits also doing the same. the aplha subunit activates the ion channel. it is inactivated by h....... of G..... to G.....
the 3 subunits recombine and attach to the receptor which can bind another agonist |
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Definition
agonist, GDP, alpha, hydrolysis, GTP, GDP |
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Term
some g proteins can stimulate or inhibit enzyme targets instead of acting on ion channels. the most common of these tragets are the enzymes: adenylate cyclase, guanylate cyclase and phospholipase C.
what are the corresponding second messengers? |
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Definition
adenylate cyclase = cyclic AMP or cAMP
guanylate cyclase = cyclic GMP or cGMP
phospholipase C = Inositol triphosphate and diacylglycerol
these can then cause a slow response in the cell |
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Term
structure of ligand gated receptors -composed of 4 or 5 different subunits arranged around a central pore. eg:nicotinic acetylcholine, GABAA, glycine, 5-HT3 receptors
nicotinic receptor has five subunits from a possible 17 thus there are many combinations that differ in skeletal muscle, autonomic ganglia,brain. the alpha subunit binds to acetylcholine resulting in a conformational change which opens the central ion channel. |
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Definition
structure of G protein coupled receptors
made from a single protein with 7 membrance spanning alpha helices = 7 transmembrane receptor (7TM)
eg: muscarinic acetylcholine, alpha-adrenergic and Beta-adrenergic receptors, all 5-HT receptors except 5HT3, rhodopsin, olfactory receptors and many others |
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Term
tricyclic antidepressants bblock noradrenaline and s.......... re-uptake
SSRIs are administered for d....... obsessive compulsive disorder and also block serotonin re-uptake |
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Definition
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Term
valium and other benzodiazepines are administered for anxiety but how do they work? |
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Definition
they activate GABA receptors
MAO inhibitors are given for Parkinson's and depression. they block the breakdown of biogenic amines. |
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Term
what is the dopamine precursor used in Parkinson's disease to cross the blood-brain barrier? |
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Definition
L dopa
acetylcholinetransferase inhibitors are administered in Alzheimer's disease to block the breakdown of acetylcholine |
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