Pharmacology Flashcards
Four categories of small molecules
Acetylcholine (ACh), monoamines, amino acids, and ATP and its byproducts
What molecule does adenosine work with?
Caffeine
Where is serotonin released?
Pons, particularly the raphe nuclei which often works with the locus coeruleus, projecting widely to the brain and spinal cord
This dopamine release circuit involves movement and sensory stimuli. It goes from the substantia nigra to the basal ganglia
Nigrostriatial
What is acetylcholines role in the PNS?
Both parts of the parasympathetic subdivision, fist part of the sympathetic subdivision, and a neuromuscular junction (NMJ)
What NT is norepinephrine made from?
Dopamine
Three indolamines
Serotonin, melatonin, and histamine
What behaviors are associated with norepinephrine?
Arousal (general state of wakefulness/excitability), vigilance, and mood
How is dopamine inactivated/removed?
Enzymes Monoamine oxidase (MAO), catechol-O-methyl transferase (COMT), and aldehyde dehydrogenase, act in sequence to break it down
Where is histamine released?
Tuberomamillary nucleus in hypothalamus
These receptors bind nicotine
Nicotinic ACh receptors
What is the main excitatory NT?
Glutamate
How does an NMDA glutamate receptor work?
Glutamate binds to AMDA receptor first, causes the NMDA to twist and the Mg+ to leave, opening the channel and allowing calcium/sodium in for a wave of depolarization
Where is glycine located?
Spinal interneurons, retina, and CNS (not usually acting independently)
What are GPCRs and what do they indicate about receptors?
G protein coupled receptors. They are metabotropic
What does noradrenaline mean?
Norepinephrine
What would serotonin pills cause?
An overactive digestive system
Where is acetylcholine released?
The basal forebrain and the cholinergic nuclei of the pons and midbrain
What does adrenaline mean?
Epinephrine
What dopamine receptors are excitatory?
D1 and D5 GPCRs (metabotropic)
What causes aggression?
Low 5HT
How is GABA made?
Made from glutamate by enzyme glutamic acid decarboxylase (GAD)
What are the functions of glycine?
Inhibition, excitation at the NMDA glutamate receptor (co-activator), and sleep
What do AMPA receptors do?
Open sodium channels. Ionotropic
What enzymes are associated with breaking down catecholamines?
Monoamine oxidase (MAO), catechol-O-methyl transferase (COMT), and aldehyde dehydrogenase
What clinical conditions/disorders are associated with norepinephrine?
Depression, anxiety, PTSD, ADHD
What is part of the catecholamines but isn’t a NT?
L-Dopa
What receptors are associated with dopamine?
D1 and D5 are excitatory
D2, D3, and D4 are inhibitory
Where is dopamine released from?
Substantia nigra (part of the midbrain) and sends to the basal ganglia. Ventral tegmentum projections to hippocampus, amygdala, and nucleus accumbens (mesolimbic). Ventral tegmentum projections to frontal lobe of the cortex (mesocortical)
What gas-transmitter easily crosses the blood-brain barrier?
Carbon monoxide (CO)
What is epinephrines role in the CNS?
Minimal. There are very few receptors in the brain.
What do NMDA receptors do and why are they special?
Opens channel for sodium and calcium. It is both voltage gated and ligand gated. Ionotropic
What are the iontropic receptors involved with glutamate?
AMPA - most common
Kainate
NMDA
What is substance P associated with?
Pain
How is glutamate removed?
Uptake into adjacent astrocytes. They change it to inactive and send it back to the axon terminal
How is GABA removed?
Uptake into adjacent astrocytes
What is cholecystokinin associated with?
Food/knowing when you’ve had enough fat
What is neuropeptide Y associated with?
Feeding/hunger/fullness
What receptors are involved with serotonin?
At least 15 different types and sub-types. Most are metabotropic and can be excitatory or inhibitory
Where is epinephrine released?
Adrenal glands near kidneys
What are oxytocin and vasopressin associated with?
Sex
What behaviors are associated with dopamine?
Movement control, reinforcement, planning, and reward
Three catecholamines
Dopamine, norepinephrine, epinephrine
How is histamine deactivated/removed?
Reuptake
What receptors do gasotransmitters interact with?
Intracellular receptors
How are catecholamines made? What must happen to make one and how are they related?
Each catecholamine is made from the one before it. They are in a series
These diffuse away from the point of release
NMs
What clinical conditions/disorders are associated with dopamine?
Parkinson’s disease (not enough=movement problems), schizophrenia, drug abuse
What is histamines role in the PNS?
In stomach to stimulate production of HCl (inc HCl to digest) and in immune system to vasodilate in response to allergies (inc mucus bc of allergies)
What are the functions of glutamate?
Excitation and long-term memory
These are released at directed synapses with a clear target in mind. They act on neurons in immediate vicinity
NTs
Three categories of neurochemicals
Small molecules, neuropeptides, and gasotransmitters
These receptors are located at NMJ (neuromuscular junction), ANS (autonomic nervous system), and CNS (central nervous system) and are excitatory and postsynaptic
Nicotinic ACh receptors
What do Kainate receptors do?
Open sodium channels. Ionotropic
How do GABA-B receptors work?
Metabotropic less common of the two. Opens potassium channels allowing it to flow out
These are released at non-directed synapses (volume-transmission) and act on distant neurons
NMs and NHs
What does L-Dopa do?
It is needed to make the other catecholamines
What receptors are involved with histamines?
H1-H4 all metabotropic GPCRs
These receptors are metabotropic/GPCR and found in myocardial, smooth muscle (digestive tract), and CNS
Muscarinic ACh receptors
What is norepinephrines role in the PNS?
Sympathetic division (fight or flight), increase blood sugar levels, increase heart rate, narrow blood vessels to increase blood pressure
Where is adenosine located?
CNS, autonomic nervous system, in cells containing catecholamines
These receptors are blocked by the poison curare
Nicotinic ACh receptors
What NTs are the primary excitatory and inhibitory NTs?
Amino acid NTs
What do indolamines always end in?
-in
This dopamine release circuit involves cognition, memory, attention, emotional behavior, and learning. It goes from the ventral tegmentum projections to frontal lobe of cortex
Mesocortical
What receptors are associated with norepinephrine?
Alpha and beta receptors
What are the functions of adenosine?
Pain modulation (reduces it) and inhibition
What behaviors are associated with histamine?
Promotes wakefulness, movement, some roles in homeostasis
What does caffeine bind to and act similarly to?
It binds to adenosine receptors and acts similar to adenosine
These travel in blood supply
NHs
Two gasotransmitters
Nitric oxide, carbon monoxide
What are some gasotransmitters and what do they do?
Nitric oxide (NO), carbon monoxide (CO), and hydrogen sulfide (H2S). They transfer info from one cell to another and diffuse through membranes and interact with intracellular receptors
What clinical conditions/disorders are associated with serotonin?
Depression, OCD, anxiety, and many more
Three amino acids and how many others (involved in neurochemicals)?
Glutamate, GABA, glycine, and 5 others
What two NTs are needed to activate an NMDA receptor?
Glutamate and glycine
What does the suffix -ergic usually tell us?
It releases a NT
What is the abbreviation for serotonin
5HT
What are the behaviors of acetylcholine?
Autonomic functions like heart rate and breathing, movement through muscle contraction, and learning/memory because it helps us to pay attention
How many neuropeptides are there?
More than 100 and counting
This dopamine release circuit involves pleasure, reward, seeking behaviors, addiction, emotion, and perception. It goes from the ventral tegmentum projections to hippocampus, amygdala, and nucleus accumbens
Mesolimbic
What is serotonins role in the PNS?
Enteric (gut) motility (biggest source of 5HT) and it is involved in everything and responsible for almost nothing
What are the receptors involved with GABA?
GABA-A and GABA-B
These receptors bind muscarine and are blocked by the poison atropine
Muscarinic ACh receptors
What do NT, NM, and NH stand for?
Neurotransmitter, neuromodulator, and neurohormone
What specific disorders or clinical conditions is ACh associated with?
Alzheimers disease because the basal forebrain is one of the first places to deteriorate due to too little ACh, myasthenia gravis due to ACh not being able to bond, and schizophrenia because many are chain smokers and nicotine binds to ACh receptors
Why are NMDA receptors good at sending a strong signal?
They let in calcium which is very positive. It is a big deal for depolarization
How is histamine synthesized?
Made from the amino acid histidine
How is serotonin synthesized?
It is made from the amino acid tryptophan
What is a special trait of gasotransmitters?
They can transmit info from postsynaptic to presynaptic neurons. They can flow forward and back.
What is dopamines role in the PNS?
Modulation. Influences the activity of a lot of other NTs
How is norepinephrine synthesized?
Dopamine beta hydroxyolase converts dopamine into norepinephrine
What are the metabotropoic receptors involved with glutamate?
mGluRs
What are the functions of GABA?
Inhibition, mood (anxiety), and seizure threshold
What is the main inhibitory NT?
GABA
These receptors mediate both inhibition and excitation in target cells and are both presynaptic and postsynaptic
Muscarinic ACh receptors
Where is norepinephrine released?
Pons (locus coeruleus which projects widely to spinal cord and brain), medulla, hypothalamus, and postganglionic sympathetic synapses
What does adenosine usually co-occur with?
Catecholamines
How is ACh removed?
Breakdown by enzyme Acetylcholinesterase (ACHE)
How do GABA-A receptors work?
Ionotropic. Cl- ion channels allows Cl- to flow in. It has many binding sites including benzodiazepines, barbiturates, and ethanol (many binding sites other than GABA)
How is dopamine synthesized?
Dopa Decarboxylase converts L-Dopa into dopamine
How is glutamate synthesized?
Kreb’s cycle
What clinical conditions/disorders are associated with histamines?
May be involved in immune system disorders or allergies or sleep disorders
How is serotonin deactivated/removed?
Reuptake by serotonin transporter and breakdown by monoamine oxidase (MAO)
What dopamine receptors are inhibitory?
D2, D3, and D4 GPCRs (metabotropic)
What is epinephrines role role in the PNS?
Increased blood sugar levels, increased heart rate, increased contractility (how hard the heart squeezes), relaxation of smooth muscle in the airways to improve breathing
What behaviors are associated with serotonin?
Mood, sleep/wake cycles, aggression, social rank, appetite
How is norepinephrine deactivated/removed?
Enzymes monoamine oxidase (MAO), catechol-O-methyl transferase (COMT), and aldehyde dehydrogenase acting in sequence to break down norepinephrine
How is ACh synthesized?
Choline from diet + Acetyl CoA enzyme choline acetyltransferase (ChAT)
Two categories of monoamines
Catecholamines and indolamines
What are endorphins associated with?
Runners high
Seven neuropeptides and how many others?
Endorphins, substance P, cholecystokinin, insulin, vasopressin, oxytocin, neuropeptide Y, and more than 40 others