Neuropharmacology Flashcards
ACh
choline + acetyl CoA - choline acetyl transferase (CAT) -> ACh (synapse, neuromuscular junction or effector tissue) -> acetyl choline esterase AChE
Muscarinic receptors mAChR
g protein, parasympathetic (target tissues), CNS modulation (memory = Alzheimers)
M1, M3
gastric function and salivary + stomach secretion via Ca (+M5 activate Gaq (Ca)) (M3= vasodilation)
M2
reduce heart rate and neuronal excitability (+ M4 inhibit Gai/o, presynapse and post)
Nicotinic receptors nAChR
sympathetic (indirectly-ganglion) parasympathetic, sodium channels (memory, cognition = ADHD, schizophrenia)
Acetylcholinesterase AChE
-> choline and acetate
NE
neurotransmitter, selective for alpha - phenylalanine, tyrosine, dopamine -> NE -> monoamine oxidase (arousal, attention, memory)
Adrenaline
hormone, selective for beta - phenylalanine -> l dopa -> dopamine -> NA -> A, locus coerulus
NET
Noradrenaline transporter, DAT - dopamine = reuptake
a1 adrenoreceptor
Gq, Ca2+, vasoconstriction (skin and GI tract)
a2 adrenoreceptor
Gi, brain, reduce presynaptic neuron NA release (modulation) via ions?
B1 adrenoreceptor
Gs, Ca2+, cardiac output and renal, CNS
B2 adrenoreceptor
Gs , v K+=hyperpolarisation, bronchodilation, vasodilation (muscular), gluconeogenesis, GI motility, CNS
B3 adrenoreceptor
Gs, adipose tissue
Glutamate
glutamine via glutaminase, taken up by astrocytes (EAAT1/EAAT2 transporters), main excitatory neurotransmitter
Group 1 metabotropic glutamate receptor
post synaptic, GqmGlu1 and 5, long term depression too much = bad, not enough =decrease brain activity
Group 2 metabotropic glutamate receptor
presynaptic, GimGlu2, 3 - prevents release
Group 3 metabotropic glutamate receptor
presynaptic, GimGlu 4, 6, 7, 8
AMPA ion channel glutamate receptor
Na, most common, activated NMDA, increase with Na2+ (LTP)
Kainate ion channel glutamate receptor
Na, post (excitatory), pre (net inhibitory via GABA increasing), hippocampus (memory and learning)
NMDA ion channel glutamate receptor
Na+Ca, LTP, both glutamate and glycine, Mg blocks, depression and schizophrenia,
LTP
long term potentiation (learning), synaptic plasticity, strengthen connection =fire at low threshold stimulus (hippocampus, amygdala), associative/specific
Excitotoxicity
too much Ca kills neurons, epilepsy - ALS disease (EAAT2), ischemic stroke (no oxygen = no ATP = depolarisation, Glutamate = neuronal cell death)
NE a1 agonist
Phenylephrine = vasoconstriction, nasal decongestant, acute hypotension
NE a2 agonist
Clonidine- (reduce NA release) = hypertension (reduce sympathetic activity), anxiety, migraine and to produce sedation
NE B blocker
Propranolol = anxiety, migraines, CV disease
NE B2 agonist
Salbutamol = asthma (relief inhalers), cause bronchodilation (salmeterol long term)
NE B1 antagonist
Atenolol, metoprolol = cardiovascular disease, including tachycardia and arrhythmias, block symp