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PPDA > Receptors > Flashcards

Receptors Flashcards

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
Q

5-HT7 (4)

A

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
Q

CB1 (4)

A

present centrally in the brain

peripherally in adipocytes, endothelial cells and peripheral nerves

Gi/o

most abundant form

27
Q

CB2 (1)

A

works peripherally on immune cells as an anti-inflammatory

28
Q

M1 (4)

A

Gq

present in the cerebral cortex

PLC - IP3 and DAG

increased cognition

29
Q

M2 (3)

A

Gi

cardiac and widely distributed in CNS

decreased cAMP, neural inhibition and tremor

30
Q

M3 (2)

A

Gq

smooth muscle and ocular accomodation

31
Q

M4 (3)

A

Gi

CNS only

increased locomotion

32
Q

M5 (2)

A

Gq

substantia nigra, salivary glands and ciliary muscles in the eye

33
Q

Noradrenaline Pathways - location, function and drugs that utilise them (3)

A 
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
Q

Conditions involving dopamine (4)

A

Parkinsons

Schizophrenia

ADHD

Drug dependence

35
Q

Locations of dopamine (4)

A

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
Q

What differs a DA neuron from a NA neuron? (2)

A

dopaminergic neurons lack dopamine-B-hydroxylase

therefore it doesnt get converted into NA

37
Q

Dopamine synthesis, reuptake, metabolism and elimination (4)

A

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
Q

Dopamine Pathways and their functions (7)

A

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
Q

Conditions involving 5-HT (6)

A

migraine

depression

anxiety

OCD

schizophrenia

drug abuse

40
Q

5-HT functions (4)

A

sleep

appetite

thermoregulation

pain perception

41
Q

5-HT synthesis (3)

A

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
Q

5-HT reuptake and metabolism (3)

A

SERT which is

inhibited by SSRIs

metabolised by MAO into 5-hydroxyindoleacetylaldehyde and then into 5-HIAA which is then excreted in urnie

43
Q

5-HT pathways (8)

A

Rostral Nucleus to the basal ganglia

cortex

hippocampus

hypothalamus

cerebellum

spinal cord

medulla

limbic system

44
Q

5-HT effects (4)

A

feeding behaviours

hallucinations

sleep and mood

control of sensory transmission - especially pain

45
Q

effect of SSRIs on appetite - what is the significance (2)

A

decreases appetite

proves SSRIs inhibit 5-HT1 receptors more than 5-hT2 receptors

46
Q

Why do hallucinogenic visions occur? (1)

A

loss of control of 5-HT pathways as these pathways normal function is to disregard irrelevant sensory informations

47
Q

Name an SSRI and an anti-psychotic 5-HT drug (2)

A

SSRI - fluoxetine

anti-psychotic - clozapine

48
Q

What is the effect of MDMA on 5-HT receptors (1)

A

competitively antagonises

49
Q

Acetylcholine is found almost everywhere except where? (1)

A

cerebellum

50
Q

What are the varieties of Ach receptor and how do the agonists and antagonists vary, and the paper that discovered it? (3)

A

(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
Q

Name non-selective muscarinic receptor agonists (3)

A

Acetylcholine

Carbechol

Bethanochol

52
Q

Name the selective M1 agonist (1)

A

McNA343

53
Q

Name the non-selective muscarinic receptor antagonists (5)

A

Atropine

Dicycloverine

Tolteridine

Oxybutinin

Hyoscine

54
Q

Selective M1, M2 and M4 antagonists? (3)

A

M1 - pirenzipine, MT7 (mambo toxin)

M2 - galamine

M4 - MT3 (mambo toxin)

55
Q

What conditions change the expression of nAchR’s (4)

A

schizophrenia

ADHD

depression

anxiety

56
Q

Which parts of the brain do CB receptors effect and what is the result? (10)

A

Hippocampus - memory and amnesia

Cerebellum - disorientation

Hypothalamus - appetite and body temperature regulation

Substantia Nigra

Mesolimbic areas - reward

Cerebral Cortex

57
Q

Explain the benefit of having limited CB receptors in the brain stem (1)

A

No serious cardiorespiratory toxic effects regarding their activation

58
Q

CB receptors have been targeted therapeutically in 8 areas of the brain, what areas and why? (18)

A

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
Q

Structure of nAchR’s (4)

A

pentameric

ligand gated cation channels

membres of the cys-lop superfamily

5-membrane spanning units form a central pore

60
Q

What is the significance of nAchR heterogenicity? (4)

A

different subtypes have different sensitivity to nicotine

different rates of discovery and desensitisation

differ in Ca++ permeability

allosteric sites and phosphorylation capabilities

61
Q

What are the functions of the brain regions?

A

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PPDA (14 decks)

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