Week 2 Flashcards
(98 cards)
What is acetyl coA synthesised from ?
Acetyl coA + Choline using the enzyme choline acetyltransferase
What is the function of acetylcholinesterase ?
Break down acetylcholine - to prevent overstimulation
What 2 main types of receptors does acetylcholine bind to ?
Nicotinic - neuromuscular junction , brain , autonomic nerves
Muscarinic - smooth muscle , exocrine glands, brain
What are some of the neuropathological changes involved with Alzheimer’s disease ?
Loss of brain weight
Enlargement of ventricles
Numerous senile plaques
Neurofibrillary tangles
How can AChE inhibitors be used as treatment for AD?
Breaks down acetylcholinesterase
More acetylcholine in the brain
What are some AChE inhibitor drugs ?
Donepezil
Rivastigmine
Galantamine
How are catecholamines synthesised ?
From tyrosine
Involves enzymes monoamine oxidase (MAO) and catechol 0-methyltransferase (COMT)
When is the mean onset of Parkinson’s disease ?
What % does it affect ?
What is it characterised by ?
60 years
1-2% of over 65 yrs
Muscle stiffness
Slowness of movement
Tremor at rest
What % of dopamine is lost usually when symptoms of Parkinson’s are recognised ?
50%
What is the reason for Parkinson’s disease ?
Degeneration of dopaminergic (DA) neurons in the substantia nigra pars compacta and loss of dopamine in the caudate-putamen
What do selective serotonin reuptake inhibitors (SSRIS) do?
What can they help reduce the symptoms of ?
What are some examples ?
block the action of SERT = more serotonin at the synapse
Depression , anxiety , OCD , PTSD etc
Citalopram
Escitalopram
Fluoxetine
Paroxetine
How is Parkinson’s disease treated ?
Motor symptoms of PD are alleviated by treatment with L-Dopa which is transported into the brain and converted to dopamine
Administration of a peripherally active Dopa decarboxylase inhibitor prevents premature conversion of L-Dopa to dopamine
Inhibitors of COMPT and MAO-B can also be given to inhibit dopamine degradation
Are amino acid transmitters non-essential or essential ?
Which are excitatory and which are inhibitory ?
Non-essential
Glutamate , aspartate - excitatory
Glycine and GABA - inhibitory
Describe GABA A and GABA B
A - ionotropic receptor coupled to Cl- channel, has modulatory binding sites for benzodiazepines , barbiturates , neurosteroids and ethanol
B - metabotropic receptor coupled to Ca2+ and K+ channels via G proteins and second messenger systems
How can memantine be helpful for treating Alzheimer’s disease ?
Blocks Mg2+ binding site on the glutamate NMDA receptor
Preventing neuronal dysfunction and cell death
Give an example of a nicotinic agonist and antagonist ?
Nicotine (tobacco) - agonist
Curare (paralysis and poison) - antagonist
Give an example of a muscarianic agonist and antagonist
Agonist - muscarine (toadstool)
Antagonist - Atropine ( deadly nightshade )
How many major families of dopamine receptors are there ?
D1- like - coupled to stimulatory G-proteins
D1, D5
D2 like - coupled to inhibitory G proteins
D2, D3, D4
What is the most common type of neurotransmitter in the hypothalamus ?
Peptide neurotransmitters
How is serotonin synthesised ?
From tryptophan by tryptophan hydroxylase and 5-hydroxytryptophan (5-HTP) decarboxylase
Broken down into 5-hydroxyindoleactic acid ( 5-HIAA) by MAO and aldehyde dehydrogenase
How many receptors and what types of receptors can serotonin bind to ?
How is action terminated ?
14
All G-protein-coupled -except for 5-HT3 which is a ligand-gated ion channel
Action terminated mainly by reuptake from the synapse via the 5-HT transporter on the pre synaptic neuron.
How is GABA synthesised from glutamate ?
Using glutamate decarboxylase
Vitamin B6
What are the different types of Glutamate receptor , what do they bind and do ?
NMDA receptor - binds glutamate , glycine , Mg2+ , Zn2+ and polyamines. Form channels that are permeable to cations
Non-NMDA receptors - Kainate and AMPA receptors interact only with glutamate and their specific agonists (Na+ , K+ > Ca2+ )
MGlut receptors - G-protein coupled receptors and trigger a second messenger cascade (eight different types of mGLuRs)