Acetylcholine

Ki

inhibition constant, concentration at red the red vertical line

when is Ki relevant?

relevant when the drug of interest blocks a process

What do tricyclics block?

the reuptake of NE and 5-HT

mechanisms which MDMA enhances acticity of 5-HT, DA, and NE

VMAT inhibition, entering, accumulation, SERT reversal, and Concentration

S-citalopram (SCIT)

SSRI which binds to SERT and inhibits MDMA binding, but does not cause large increases in 5-HT

Did SCIT treatment alter social preference?

prevented the increase in social approach normally elicited by MDMA

how is serotonin involved in pain reductions?

via endorphins

where is serotonin release in regards to pain reduction?

the spinal cord neurons, which release endorphins

what does presynaptic inhibition of of endorphins cause?

less release of substance P by the pain fiber

what does the term endorphins “gate” mean?

to turn down the ‘volume of’

what are low serotonin levels associated with?

aggression, violent behavior, and psychopathy

what is the MAOA sequence related to?

sensitivity to early life experiences

acetylcholine synthesis

Choline+AcetylCoA»Choline acetyltransferase» Acetylcholine+Coenzyme A

Acetylcholine breakdown

Acetylcholine»acetylcholinesterase»Choline+Acetic acid

Where can acetylcholinesterase(AChE) be found?

pre-synaptic axon terminal, post-synaptic membrane, in the “synapse” at the neuromuscular junction

Which organs exclusively receive sympathetic nervous system intervention?

adrenal gland, sweat gland

what does stress lead to? (1st basis for lie detector test)

lead to sweating via sympathetic activation(Ex: sweaty palms)

effects of atropine and scopolamine

dialated pupils, inhibits salivation, prevents cardiac slowing

where is atropine found?

found in the belladonna plant(rennaisane)

Can atropine and scopolamine cross the BBB?

only scopolamine

what is scopolamine used to treat?

motion sickness

motor neuron

alpha motor

neuron

lower motor neuron

myasthenia gyrus

autoimmune destruction of acetylcholine receptors

what is used to treat myasthenia gravis?

acetylcholinesterase(AChE) blockers, like pyridostigmine and immunosuppressants

what does botulinum toxin prevent?

vesicle fusion at the neuromuscular junction

what does botulinum toxin block?

the exocytosis of acetylcholine

2 main subtypes of cholinergic receptors

muscarinic and nicotinic

how many subunits do nicotinic receptors have?

5

what state can a nicotinic receptor enter?

desensitized

suxamethonium

long-lasting muscle relaxant that works by initially stimulating the receptors, but then causes them to enter the desensitized state

what does sarin nerve gas cause?

profuse sweating and salivation, vomiting, and convulsions

what does sarin nerve gas affect?

AChE

muscarine and pilocarpine are agonists for..?

muscarinic receptor

where can you find muscarine and pilocarpine?

poisonous mushrooms

what do muscarine and pilocarpine cause?

sweating and salivation, pupil constriction, and decreased heart rate

what does the postganglionic sympathetic cholinergic fibers innervate?

eccrine sweat glands(cooling)