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Receptors Flashcards

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1
Q

GABAa (11)

A

involved in chloride inhibition

post synaptic

formed from varying subunits 2a2by

6a subunits, 3b subunits, 3y subunits

BZDs dont work on a4-6 subunits

a5 subunit involved in memory

Binding site between a and y is BZDs

binding site between a and b is agonists/antagonists

channel blockers block the middle of the channel

allosteric modulators (barbiturates) are in the middle of the channel

channel modulators bind to the interior of the channel

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2
Q

GABAb (4)

A

pre and post synaptic

GPCR linked Gi/Go

K+ cascade

effected by GHB when in high concentrations

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3
Q

GHB (1)

A

stimulated in low concentrations of barbiturates and increases dopamine and alertness

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4
Q

AMPA (4)

A

post synoptic

must be activated before NMDA in order to remove Mg++

Glutamate receptors 1-4 are AMPA

ligand gated ion channel

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5
Q

Kainate (4)

A

pre and post synoptic

must be activated before NMDA in order to remove Mg++

glutamate receptors 5-7 are kainate
K1-2

ligand gated ion channels

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6
Q

NMDA (3)

A

post synaptic

heterotetrameric structure

ligand gated ion channel

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7
Q

a1 (6)

A

Gq

NA > A > IA

agonist - phenylephrine and methoxamide

antagonist - prazosine and dozazocine

PLC breaks PIP2 to IP3 and DAG causing Ca+ release

in charge of motor control, cognition and fear

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8
Q

a2 (6)

A

Gi

A > NA > IA

agonist - clonidine

antagonist - yohimbine and lolazoxan

inhibits sympathetic flow of CNS, decreases cAMP and Ca++ and increases K+

present in all CNS terminals

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9
Q

b1 (6)

A

Gs

IA > NA > A

agonist - dobutamine

antagonist - atenolol, and metaprolol

increases cAMP

present in cortex, striatum and hippocampus

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10
Q

b2 (6)

A

Gs

IA > A > NA

agonists - salbutamol, turbutaline, salmeterol and clenbuterol

antagonists - butoxamine

inhibits histamine release from mast cells and increases cAMP

found in the cerebellum

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11
Q

D1 (6)

A

Gs

agonist - dopamine

partial agonist - apomorphine and bromocryptane

antagonist - clorpromazine, haloperidol and clozapine

involved in reward pathways that produce Euphoria (Sibley 1999)

expressed highly in the cortex, limbic systems and striatum

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12
Q

D2 (6)

A

Gi/Go

agonist - dopamine, apomorphine and bromocryptane

antagonists - chlorpromazine, haloperidol, spiperone, roclopride

expressed highly in cortex, limbic system, striatum, ventral hypothalamus and anterior pituitary

present in chemoreceptor trigger zone in the medulla associated with N&V

decreased Ach increases K+ and decreases Ca++ which activates pre and post synpatic inhibiton

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13
Q

D3 (5)

A

Gi/Go

agonist - dopamine, apomorphine and bromocryptane

antagonist - spiperone, haloperidol and clorpromazine

high in limbic system, striatum, ventral hypothalamus and anterior pituitary

decreased Ach increases K+ and decreases Ca++ which activates pre and post synpatic inhibiton

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14
Q

D4 (5)

A

Gi/Go

agonist - dopamine, apomorphine and bromocryptane

antagonist - haloperidol, spiperone and clozapine

high in limbic system and striatum

decreased Ach increases K+ and decreases Ca++ which activates pre and post synpatic inhibiton

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15
Q

D5 (4)

A

Gs

high in limbic system and striatum

agonist - dopamine, apomorphine and bromocryptane

antagonist - clorpromazine, haloperidol and clozapine

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16
Q

I1 (2)

A

receptor for imidazoline

inhibition of sympathetic nervous system to decrease BP

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17
Q

I2 (2)

A

receptor for imidazoline

allosteric binding site on MAO - psychiatric association

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18
Q

I3 (2)

A

receptor for imidazoline

insulin secretion regulation

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19
Q

5-HT1 (6)

A

inhibitory

1A - widely distributed in the limbic system and is the major target for anxiety and depression meds

5-HT1A was found to control feeding behaviour by increasing appetite

1B and 1D - presynaptic inhibitory in the basal ganglia and cortex

5-HT1D antagonist sumatriptan - used for migraines

agonised by Bisporone as a treatment for anxiety

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20
Q

5-HT2 (5)

A

LSD acts upon it

inhibitory and excitatory by glutamate and GABA balance

2A and 2C - abundant in cortex and limbic system

Barnes + Sharp 1999 found that hallucinations and behavioural changes are by 5-HT2A

5-HT2 receptors have been found to decrease appetite

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21
Q

5-HT3 (4)

A

ligand gated ion channel (homo/heteromeric, Peters et Al 2005)

present in the area postrema causing vomiting

role of 3A and 3B is known Jensen et Al 2008

antagonised by ondansetron - use as an antiemetic

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22
Q

5-HT4 (3)

A

present in the limbic system, basal ganglia, hippocampus, substantia nigra

increased cognitive performance by increasing Ach release

receptors oppose respiratory depression actions in opioids

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23
Q

5-HT5 (1)

A

Baekaert et Al 2006 presented conflicting information on location and function

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24
Q

5-HT6 (2)

A

present in the hippocampus, cortex and limbic system

are targets for increased cognition and schizophrenia

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25
5-HT7 (4)
LSD acts upon it present in hippocampus, cortex, amygdala, thalamus and hypothalamus found on axon terminals of GABAergic neurons thermoregulatory systems, endocrine and mood, cognitive function and sleep
26
CB1 (4)
present centrally in the brain peripherally in adipocytes, endothelial cells and peripheral nerves Gi/o most abundant form
27
CB2 (1)
works peripherally on immune cells as an anti-inflammatory
28
M1 (4)
Gq present in the cerebral cortex PLC - IP3 and DAG increased cognition
29
M2 (3)
Gi cardiac and widely distributed in CNS decreased cAMP, neural inhibition and tremor
30
M3 (2)
Gq smooth muscle and ocular accomodation
31
M4 (3)
Gi CNS only increased locomotion
32
M5 (2)
Gq substantia nigra, salivary glands and ciliary muscles in the eye
33
Noradrenaline Pathways - location, function and drugs that utilise them (3)
``` Locus Coerulus to the cerebellum Locus Coerulus to the Cortex Locus Coerulus to hypothalamus Locus Coerulus to the hippocampus Locus Coerulus to the spinal cord ``` antidepressants, cocaine and amphetamines arousal, blood pressure regulation and mood
34
Conditions involving dopamine (4)
Parkinsons Schizophrenia ADHD Drug dependence
35
Locations of dopamine (4)
most abundant in the corpus striatum - motor system for coordination and movement high also in frontal cortex high in limbic system high in hypothalamus
36
What differs a DA neuron from a NA neuron? (2)
dopaminergic neurons lack dopamine-B-hydroxylase therefore it doesnt get converted into NA
37
Dopamine synthesis, reuptake, metabolism and elimination (4)
same pathway as NA for sytnehsis reuptake by DAT metabolism by MAO and COMT COMT converts to DOPAC and HVA (which is an indicator of DA turnover) released in urine as an indicator for DA release in body
38
Dopamine Pathways and their functions (7)
Nigrostriatial - 75% of dopamine neurons Substantia Nigra - corpus striatum via the medial forebrain bundle motor control Mesolimbic VTA (in pons cluster) - amygdaloid nucleus via the medial forebrain bundle Behavioural control and emotion Mesocortical VTA to the frontal cortex Tuberohypophyseal Hypothalamus to the pituitary Endocrine functions - inhibit prolactin release
39
Conditions involving 5-HT (6)
migraine depression anxiety OCD schizophrenia drug abuse
40
5-HT functions (4)
sleep appetite thermoregulation pain perception
41
5-HT synthesis (3)
PCPA can selectively and irreversibly inhibit Tyrptophan Hydroxylase Availability of trytophan varies by food intake and time of the day as its derived by dietary protein Tryptophan hydoxylases are the main factors to regulate synthesis
42
5-HT reuptake and metabolism (3)
SERT which is inhibited by SSRIs metabolised by MAO into 5-hydroxyindoleacetylaldehyde and then into 5-HIAA which is then excreted in urnie
43
5-HT pathways (8)
Rostral Nucleus to the basal ganglia cortex hippocampus hypothalamus cerebellum spinal cord medulla limbic system
44
5-HT effects (4)
feeding behaviours hallucinations sleep and mood control of sensory transmission - especially pain
45
effect of SSRIs on appetite - what is the significance (2)
decreases appetite proves SSRIs inhibit 5-HT1 receptors more than 5-hT2 receptors
46
Why do hallucinogenic visions occur? (1)
loss of control of 5-HT pathways as these pathways normal function is to disregard irrelevant sensory informations
47
Name an SSRI and an anti-psychotic 5-HT drug (2)
SSRI - fluoxetine anti-psychotic - clozapine
48
What is the effect of MDMA on 5-HT receptors (1)
competitively antagonises
49
Acetylcholine is found almost everywhere except where? (1)
cerebellum
50
What are the varieties of Ach receptor and how do the agonists and antagonists vary, and the paper that discovered it? (3)
(a4)2(B2)3 - agonist is nicotine and epibatidine antagonist - mecamylamine (a7)5 - agonist is epibatidine antagonist - a-bungarotoxin and a-comotoxin discovered by Gotti et al, 2008
51
Name non-selective muscarinic receptor agonists (3)
Acetylcholine Carbechol Bethanochol
52
Name the selective M1 agonist (1)
McNA343
53
Name the non-selective muscarinic receptor antagonists (5)
Atropine Dicycloverine Tolteridine Oxybutinin Hyoscine
54
Selective M1, M2 and M4 antagonists? (3)
M1 - pirenzipine, MT7 (mambo toxin) M2 - galamine M4 - MT3 (mambo toxin)
55
What conditions change the expression of nAchR's (4)
schizophrenia ADHD depression anxiety
56
Which parts of the brain do CB receptors effect and what is the result? (10)
Hippocampus - memory and amnesia Cerebellum - disorientation Hypothalamus - appetite and body temperature regulation Substantia Nigra Mesolimbic areas - reward Cerebral Cortex
57
Explain the benefit of having limited CB receptors in the brain stem (1)
No serious cardiorespiratory toxic effects regarding their activation
58
CB receptors have been targeted therapeutically in 8 areas of the brain, what areas and why? (18)
Basal ganglia and cerebellum treatment of motor function disorders such as MS Hippocampus treatment for memory and learning disorders Cerebral cortex treatment of higher cognitive function loss Hypothalamus treatment of depression and obesity disorders as CB has effects on thermoregulation, endocrine function and appetite Amygdala treatment of depression emotion centre Spinal Cord treatment for peripheral sensation and chronic pain Brain stem to treat N&V as it has no specific area postrema receptors cancer patients
59
Structure of nAchR's (4)
pentameric ligand gated cation channels membres of the cys-lop superfamily 5-membrane spanning units form a central pore
60
What is the significance of nAchR heterogenicity? (4)
different subtypes have different sensitivity to nicotine different rates of discovery and desensitisation differ in Ca++ permeability allosteric sites and phosphorylation capabilities
61
What are the functions of the brain regions?
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