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Neur 201 > Module 3 - Neuropharmacology > Flashcards

Module 3 - Neuropharmacology Flashcards

(102 cards)

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1
Q

Why are GPCR’s important in Pharmacology?

A

About 50% of drugs target GPCR’s. 5 out of 20 of the most commonly prescribed drugs in NZ target GPCR’s. 95% of psychiatric drugs in NZ directly or indirectly target GPCR’s

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2
Q

What do DAG and IP3 do?

A

IP3 increases free Ca from the ER, DAG activate protein Kinase A

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3
Q

What secondary messengers do Adenylyl cyclase and phospholipase C activate?

A

cAMP (intracellular signalling molecule, activates protein kinase A), Phospholipase C breaks down molecules in cell membrane into DAG and IP3

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4
Q

GPCR signalling leads to the deactivation or activation of what enzymes?

A

Adenylyl cyclase and phospholipase C

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5
Q

What is the process of GPCR activation?

A

Agonist binds causing conformation change in receptor shape. This allows GTP to replace GDP on alpha subunit. GTP bound alpha subunit breaks away from receptor and interacts with a target protein to modify cell signalling.

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6
Q

What is quicker ion channels or GPCR’s?

A

Ion channels

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7
Q

What are the two G proteins?

A

Gs and Gi

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8
Q

What does Gs do?

A

Dopamine type 1 (D1) receptor has a Gs subunit. Activates Adenylyl cyclase, amplifies cAMP which activates PKA (activates Na channels)

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9
Q

What does Gi do?

A

Dopamine type 2 receptor has a Gi subunit, deactivates Adenylyl cyclase, decreases cAMP, Activates potassium ion channels (GIRK), Closes calcium channels.

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10
Q

Where are muscarinic type 3 receptors found?

A

intestinal smooth muscles cells.

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11
Q

When activated by Ach what do M3 receptors do?

A

activate PLC which produces IP3, releases Ca from SR. Ca binds to calmodulin. Calmodulin activates myosin light chain kinase. Phosphorylation myosin light chains and muscle contraction

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12
Q

What are common forms of GPCR’s?

A

Cannabinoid, Adenosine, Serotonin, Dopamine, Alpha, Opioid. Muscarine.

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13
Q

What is an example of a GPCR’s psychological effects?

A

Opioid receptors are found in the brain stem, on neurons that transmit pain signals. Opioids activate Gi couples GPCR’s activating GIRK and closing Ca channels, Neuron doesn’t fire, pain signal stops and pain is not perceived.

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14
Q

What are biological targets of drugs?

A

Receptors (Caffeine), Enzymes (Acetylcholinesterase inhibitors) and Transporters (methylphenidate).

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15
Q

What are agonists?

A

Drugs that increase receptor activity by causing a change in shape when they bind

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16
Q

Where do drug agonists typically bind?

A

typically bind in the same area as endogenous biological agonists (ligands). e.g. nicotine or morphine and can sometimes fit better then the body’s natural agonist.

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17
Q

What is a drugs ability to properly bind to a receptors known as?

A

Affinity

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18
Q

What kind of physiological response would a full agonist produce?

A

A maximal physiological response (e.g. increasing heart rate to biological maximum, 200 BPM)

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19
Q

What kind of physiological response would a partial agonists produce?

A

Would cause a response below the maximal response.

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20
Q

How is biological response measured?

A

Sometimes easy e.g. blood pressure or heart rate, or hard e.g. anxiety or depression. Effect size is a common way to determine efficacy of drugs.

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21
Q

What is an antagonist?

A

Antagonists work by decreasing activity of a receptor in the presence of an agonist. They have no effect on their own as they cannot activate receptors (no efficacy)

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22
Q

Where does adenosine come from?

A

Made as a result of the breakdown of ATP

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23
Q

what kind of Agonist is caffeine?

A

An Adenosine Receptor Agonist. Works by decreasing intracellular cAMP which can decrease neuron firing

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24
Q

What is the caffeine mechanism of action?

A

throughout the day the buildup of adenosine activates adenosine receptors (A1). Caffeine binds to A1R preventing adenosine from binding. this increases cAMP and prevents hyperpolarisation.

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25
What effects does coffee have?
In a rested state caffeine causes improvements in some areas of cognition. In a sleep derived state caffeine causes larger improvements in aspects of cognition including (information processing, reaction time, driving test scores).
26
How do drugs which target enzymes work?
Stop enzymes from working (enzyme inhibition), Leads to the buildup of endogenous enzymes. Many drugs can inhibit liver enzymes as a side effect e.g. Fluoxetine and bupropion inhibit CYP2D6
27
Which psychological disorder treating drugs target receptors?
SSRI's e.g. Fluoxetine, Or NDRI's for ADHD (Ritalin)
28
What do PAM's do?
increase receptor activity when the endogenous agonist binds
29
What kind of receptors does Ach bind to?
Ligand gated ion channels, GPCR's (Gi and Gq)
30
Ach regulates what parts of the immune system?
SNS (Indirectly) and PNS (Directly)
31
What actions does Ach have in the PNS?
Activates nicotinic receptors in the ganglion and activates muscarinic receptors at the target tissues.
32
What actions does Ach have in the SNS?
activates nicotinic receptors in the ganglion. Noradrenaline and Norepinephrine activate alpha and beta receptors in the target organs. nAchR in the adrenal gland leads to systematic release of NE/NA.
33
Muscarinic receptors 1,3 and 5 effect what?
Gq - coupled GPCR's
34
Where are M1,3 and 5 receptors found?
M1 receptors are found in the brain, salivary glands and tear ducts. M3 found in Smoot muscle of GI M5 found in the eye and brain
35
Muscarinic receptors 2 and 4 effect what?
Gi - couples GPCR's
36
Where are M2 and 4 receptors found?
M2 found in the heart and brain M4 is found in the brain
37
What actions does the activation of M3 cause?
M3 activation activates PLC, producing DAG and IP3, increasing intracellular Ca and causing a GI muscle contraction.
38
What action does the activation of M2 cause?
M2 activation decreases cAMP activity, prevents PKA from activating calcium channels, calcium doesn't enter cell, decrease in contractility of the heart, decreases heart rate.
39
What action the activation of M4 have?
Schizophrenia caused by to much dopamine in the VTA, M4 receptors inhibit neurons from firing, preventing release of Ach. less activation of nicotinic receptors, less depolarization of dopaminergic neurons in the VTA, decreases schizophrenia symptoms.
40
What are muscarinic agonists (drugs) for schizophrenia?
Clozapine most effective, but many bad side effects, Xanomeline also used but less effective.
41
What are xanomeline's properties and uses?
Is a non-selective agonist. Often used Post anaesthesia to stimulate GI activity and bladder emptying. Used to treat Atrial Tachycardia
42
What is a antagonist of the PNS?
Non-selective competitive antagonists such as tropsium, atropine, hyoscine are used in eye exams, prevent slowing of HR, salivary and bronchial secretions (not good for asthma), reduced intestinal spasm, motion sickness, brachycardia and insecticides.
43
what are examples of natural anticholinergics?
Atropa belladonna, Mandrake, Jimson weed,
44
What is the structure and function of nAchRs?
ligand gated ion channels. present in sympathetic and parasympathetic ganglia, when Ach binds channel opens causing effects throughout CNS.
45
The Somatic nervous system connects the Central Nervous system directly to what?
Skeletal muscle
46
What is the process of nAchR desensitisation?
prolonged opening leads to desensitisation, Calcium is taken up by ER, muscle relaxation occurs
47
Ach is degraded by what?
Acetylcholinesterase.
48
What are Acetylcholinesterase (AchE) inhibitors?
E.g. Donazepil, Reduced Ach breakdown at synapses used for Alzheimer's disease and treating muscle relaxants.
49
What are treatments for Alzheimer's disease?
target two main transmission pathways, Glutamate antagonists at NMDA receptors or acetylcholinesterase inhibitors (Donazepil).
50
What are irreversible AchE inhibitors?
Insecticide poisons (organophosphates), Nerve agents (VX agent and novichok). Parasympathetic effects occur first followed by sympathetic.
51
What is Noradrenaline (Norepinephrine) ?
Neurotransmitter of the SNS, active when the individual is at rest.
52
What is adrenaline (epinephrine) ?
hormone released from the adrenal gland in response to SNS activation
53
What does SNS activation lead to?
increases in HR and sweating, inhibits secretion and GI motility, Bronchodilation, vasoconstriction and dilation, enhanced neuronal activity
54
What do a1 adrenergic receptors do?
mediates smooth muscle contraction in the skin. Gq coupled GPCR. Increase Ca concentration causing vasoconstriction
55
What are a1 adrenergic agonists?
phenylephrine, adrenaline, noradrenaline which are used as nasal decongestants
56
Where is Noradrenaline found in the brain?
Released from the Locus Coerulus, activity high during the day or anxiety and low while asleep.
57
What is Noradrenaline's function in the brain?
increased arousal, enhanced attention, formation and retrieval of memories and processing sensory inputs, Low levels in the prefrontal cortex associated with ADHD
58
What is ADHD?
Predominately classified by inattentive or hyperactive-impulsive subtypes. 6& of children and as much as 16% of adults. 2 fold increase in mortality. Low levels of noradrenaline and Dopamine in prefrontal cortex
59
What are the four main ways drugs treat ADHD?
Inhibit reuptake of Noradrenaline and Dopamine (methylphenidate). inhibit noradrenaline reuptake only (Atomoxetine). Facilitate the release of Noradrenaline and Dopamine (Amphetamine). A2noradrenaline receptor agonists (Guanfacine).
60
What do D1 receptors do?
Activation enhances neurotransmission of relevant stimuli. drugs that increase dopamine neurotransmission are called stimulants.
61
What are Non pharmalogical treatments for ADHD in children?
Exercise and Cognitive Behavioural Therapy
62
What do NET and DAT reuptake inhibitors do?
remove NA/DA from the synapse
63
What are A2 agonists?
can directly enhance some aspects of cognition. Drugs include Guanfacine and Clonidine
64
What do Amphetamines do?
binds to reuptake transports and vesicle storage proteins causing release Dopamine and NA in cytoplasm. increase activation without the LC e.g. lisdexamfetamine
65
What are pharmacological treatments for anxiety?
Noradrenergic modulators (beta blockers (propranolol) and clonidine) Benzodiazepines (effective and commonly prescribed anxiolytics but are often abused)
66
What type of beta blocker is propranolol?
non selective B1 and B2 antagonist, particularly useful in performance anxiety, reduces SNS effects.
67
What are benzodiazepines?
positive allosteric modulator for GABAa. Increases frequency of channel opening when GABA binds. Increases hyperpolarization of neurons. decreases general neurotransmission throughout the brain.
68
What is tolerance?
a decrease in the potency of a drug after repeated use.
69
What are the causes of tolerance?
Change in receptor function (e.g. desensitisation). internalisation of receptors and transporters. Exhaustion of mediators. increased drug metabolism.
70
What is receptor downregulation?
fewer receptors are available on the postsynaptic neurons. Neurotransmitter release results in less receptor activation.
71
What are the receptors involved in drug abuse?
Dopamine, Alpha (noradrenaline), serotonin, NMDA (Glutamate), Opioid, GABA, Cannaboid, Nicotinic (Acetylcholine)
72
What behavioural addictions is dopamine believed to be involved in?
Gambling, Food, Sex
73
What areas of the brain is Dopamine found and secreted?
Dopamine found in the VTA and dopamine receptors are found in the nucleus accumbens.
74
Most addictive drugs cause an increase of what in the brain?
Dopamine
75
MDMA releases neurotransmitters the same way as what other drug?
Methamphetamines, MDMA is also much less likely to cause dependance.
76
Methamphetamine enters the brain quicker then what other drug?
Amphetamines
77
What are NDRA's and SRA's?
Noradrenaline and Dopamine releasing agents and Serotonin releasing agents.
78
What type of drug is cocaine?
A noradrenaline and Dopamine reuptake inhibitor
79
What effect does speed have on drug absorption?
makes them more likely to imitate the phasic release of dopamine
80
Why does the speed of administration matter?
D1 receptors have a lower affinity than D2, D1 is responsible for the dopamine high. Rapid delivery activates more D1
81
Which drug causes rapid dependence?
Amphetamines
82
Which drug causes stringer psychological dependence than physical dependence?
Cocaine
83
What type of drug is MDMA?
A serotonin releasing agent (agonist)
84
What are problem with serotonin agonists?
They exhibit rapid tolerance, psychedelics such as LSD show lower user dependence
85
Hallucinogens are agonists for what?
The 5-HT2a Receptor, Gq coupled receptors, Tolerance rapidly developes but dependence is very rare.
86
What are examples of Depressants?
Alcohol and Benzodiazepines, they hyperpolarise neurons and can stimulate certain brain areas. Is hard to overdose
87
What is the mechanism for alcohol?
Alcohol is a positive allosteric modulator for GABAa
88
Alcohol increases the firing rate of neurons where?
In the VTA causing dopamine release in the Nucleus accumbens. Alcohol increases the release rate of opioids in the brain.
89
What is the Tolerance process of GABAa receptors?
Fewer receptors receive Cl influx meaning less hyperpolarisation of neurons and increased excitable activity.
90
How is opioid euphoria modulated?
modulated in mu-opioid receptor, Diamorphine (Heroine) has similar effect intravenously, Codeine doesn't
91
What are the opioid withdrawal symptoms in mice?
irritability, Diarrhoea, Weight loss, Abnormal behaviour patterns (Shaking, writhing, aggression)
92
What are the three main opioid receptors?
Mu-opioid (euphoric effects), Delta-opioid and Kappa-opioid
93
What is a analgesic?
Drug that relieves pain without effecting other senses. Anaesthetic impairs senses.
94
What are the two main analgesic types?
NSAID (non-steroidal anti-inflammatory drug) and Opioids
95
What is nociceptive pain?
Pain from direct simulation of pain receptors. Is transmitted along normal, healthy neurons to the brain. Tissue injury apparent. Treated with NSAIDS or Opioids.
96
What is neuropathic pain?
From injured peripheral or central nerves. Can result from trauma. Pain can occur without obvious injury. Management is different to nociceptive.
97
What is acute or chronic pain classified as?
Acute pain (Identified event, resolved in days to weeks, typically nociceptive) Chronic pain (cause not easily identified, often multiple factors, indeterminate duration, nociceptive or neuropathic)
98
How do opioids cause analgesia?
Acts in the brain and spinal cord as a pain inhibitory system. blocks the transmission and perception of pain. Gi couples GPCR's stop neurons sending pain signals.
99
How is pain perceived in the brain?
Pain signals travel up spinal cord to the thalamus. Thalamus sends pain signals to the somatosensory cortex. This is where pain is perceived.
100
Where are opioid receptors found in the brain?
Highly concentrated in the brain. Found in VTA/nucleus accumbens. Receptors in the brain stem supress breathing response.
101
What are the symptoms of Opioid Dependence?
Withdrawal symptoms (Fever, Diarrhoea, Sweating, nausea, insomnia and pain),
102
What is Tramadol's uptake mechanism?
mu-opioid receptor prodrug (metabolised by CYP2D6), Serotonin and Norepinephrine reuptake inhibitor.

Neur 201 (4 decks)

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