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35 Cards in this Set

  • Front
  • Back

How does cocaine addiction affect the makeup of the nervous system?

Increase in dendritic spinal density




Sensitisation of neurons through the upregulation of the gene MEF2.

What do optogenetics in mice show?

Shows that newly acquired motor skill depends on the formation of task specific dense synaptic ensembles

What effect does the alkaloid "Muscarine" have on the body?


What species is it from?

Slows heart rate.


Amanita muscarina

What effect does the alkaloid "Atropine" have on the body?


What species is it from?

Alkaloid which blocks the actions of muscarine and shows vagal stimulation.


Deadly Nighthase - Atropa belladonna

What effect does nicotine have on the body?

Stimulates contraction of skeletal muscles.

What effect does 'Curare' have on the body?


In the past whats was this used for?

Blocks action of nicotine and the neuromuscular junction.


Used as the poison on the tip of poison arrows of SA indians.

What processes can be targeted in the pre synaptic knob for inhibition?


Give an example of a molecule or group of molecules which block each.

1. Acetlycholine (ACh) carrier inhibition - so ACh vesicles are not shuttled to the membrane - Vesamicol


2. Acetylcholine exocytosis inhibition - Presynaptic toxins


3. Choline carrier inhibition to prevent reuptake of choline into the presynaptic knob - hemicholinium


4. Inhibition of the pre-synaptic nicotinic ACh receptor - Non depolarising blocking agents

What are the effects of tetanus in the nervous system and thus on the wider body?

Prevents fusion of vesicles wit h the presynaptic membrane. Functions on inhibitory neurons so increases muscular contraction.

What processes can be targeted in the post synaptic knob & synaptic cleft for inhibition?


Give an example of a molecule or group of molecules which block each.

1. Acetylcholinesterase inhibition - prevents breakdown of acetylcholine - Neostigmine, Sarin


2. Non Depolarising Blocking Agents - prevent fusion of acetylcholine to the post synaptic ligand bound receptors.


3. Depolarising blocking agents which mimic acetylcholine but are not broken down by acetylcholinesterase - succinylcholine.

What are the effects of sarin in the nervous system and thus on the wider body?

Sarin is a nerve gas which inhibits acetylcholinesterase. This results in uncontrolled muscle contraction.

What are the effects of tetrodotoxin in the nervous system and thus on the wider body?

Binds to voltage gated sodium channels and prevents action potentials from forming. Results in paralysis.

What type of receptor are muscarinic receptors?

G - Protein coupled



Where are muscarinic receptors found?

Post-ganglionic parasympathetic nerve terminals.

How many types of Muscarinic receptors are there?


What is the nomenclature?

5 types - M1, M2, M3, M4, M5

What is another name for M1 receptors?

Neural

What G protein types make up M1 receptors?

Gi, Gs & Gq

Where are M1 receptors found?


How are they signalled?



1. Mainly found in the CNS


2. Signalled via IP3 / Ca2+ pathway and inhibition of K+ channels

What is another name for M2 receptors?

Cardiac

What G protein types are M2 receptors?

Gi

Where are M2 receptors found?


How are they signalled?


What is their effect?

1. Mainly in the heart and some in the CNS


2. Signal via cAMP inhibition and activation of K+ channels


3. Effect: slows the speed of depolarisation

What is another name for M3 receptors?

Glandular / Smooth muscle receptors

What G protein type are M3 receptors?

Gq

Where are M3 receptors found?


What physiological responses do they promote?

1. Mainly glands and smooth muscle


2. Promotes glandular secretion, vasoconstriction of the lung and vasodilation of the blood vessles.

Where are M4 and M5 receptors found?


What G protein types are they?

1. Mainly in the CNS


2. M4 - Gi


M5 - Gq

What is the drug type which stimulate muscarinic receptors termed?


And inhibits?



1. Parasympathomimetics - effects resemble PS system stimulation


2. Parasympatholytics - effects reverse of PS system

What drug can be used to target M3 receptors?


What effect does this have?

1. Bethanechol

2. Clinically used to relieve bladder + GI hypotonia


What drug can be used to treat glaucoma?

Pilocarpine

How specific are most muscarinic receptor agonists?

Most are non selective for the M1 - M5 subtypes

What are the cardiovascular effects of muscarinic agonists.

1. Bradycardia (BPM <60)


2. Low Cardiac output


3. Vasodilation - lowers blood pressure

What are the effects of muscarinic agonists on smooth muscle?


What physiological effects does this have?

1. Contraction of smooth muscle except vascular smooth muscle


2. - increase in peristaltic activity, bladder contraction, constriction of bronchioles



What are the effects of muscarinic agonists on the eye?


What is the key physiological effect this has?

1. Pupil constriction


2. Constriction of the ciliary muscle - decrease in intraocular pressure (perfect for treating glaucoma)

What are the effects of muscarinic agonists on glands and the central nervous system?

Increase in glandular secretion.




'Central' effects:


1. Tremor


2. Hypothermia


3. Increased locomotive activity


4. Improved cognition

What are the clinical uses of muscarinic agonists?

Main: For treating glaucoma


Secondary: Dry eye & mouth


Rare: Urinary retention - bethanechol

How would you treat urinary retention or weak muscles in the GI tract?


What are its side effects?

Bethanechol




Side effects:


1. Sweating


2. Blurred vision


3. Bradycardia

What is the drug used by opticians to make pupils dilate?


What is the effect on muscarinic receptors?

1. Atropine


2. Is a muscarinic antagonist.