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Receptors and ion channels > Receptors > Flashcards

Receptors Flashcards

1
Q

What is a receptor

A

A protein that recognises and creates a response to Environmental stimuli

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2
Q

Receptor classes

A

Ligand gated ion channel(Inotropic)
G protein coupled receptors(metabotropic)
Kinase linked
Nuclear receptors

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3
Q

Agonist

A

A chemical that binds to a receptor to activate it causing a biological response

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4
Q

Active AR complex

A

Agonist+receptor= Active AR complex

causes a conformational change in the receptor causing agonist induced response

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5
Q

Drug Agonist types

A

Full agonist-Receptor fully activated

Partial agonist-Activates receptor partially

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6
Q

Affinity

A

The strength in attraction between the receptor and the agonist.
Smaller kd means higher affinity

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6
Q

Efficacy

A

The maximum biological affect(Emax)

Partial agonist have low efficacy

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7
Q

Potency

A

Potency is the concentration required to reach 50% of maximal effect(EC50)
Depends on the affinity

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8
Q

Anxiolytic affect

A

When partial agonist binds it causes anxiolytic affect therefore having anti anxiety affect whereas a full agonist has sedation effect

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9
Q

Inverse agonist

A

Binds to the same receptor as an agonist but induces an effect opposite to an agonist. It occurs to the receptors with constitutive activity(basal activity)

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10
Q

Spare receptors

A

receptors that exist in excess of those required to produce a full effect

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11
Q

Antagonist

A

A receptor that binds to a receptor but does not activate it

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12
Q

Antagonist classes

A

Reversible-Competitive/non-competitive

Irreversible

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13
Q

How to overcome competitive antagonist

A

Increasing agonist concentration or decreasing antagonist

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14
Q

Competitive antagonist effect

A

Parallel shift to the right but no change to slope

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15
Q

Schild Plot

A

Schild Plot is used to compare the different affects of the antagonist to the receptor.

16
Q

PA2

A

Shows how competitive an antagonist is
If there is a competitive agonist the slope should be 1
You can also tell how potent and effective the antagonist is
The smaller the PA2 the better it binds to the receptor

17
Q

Non-competitive antagonist

A

binds to the allosteric site

Haxamethonium blocks the ion channel of the nicotinic receptor

18
Q

Irreversible competitive antagonist

A

This antagonist dissociate very slow from the receptor
Increasing concentration does not increase response
Binds to the receptors using covalent bonds

19
Q

Irreversible competitive antagonist as non-surmountable

A

The inhibition is non-surmountable(The proportion of receptors occupied by the antagonist is lost by the agonist
Maximum response is decreased

20
Q

Specificity

A

Measures how well a drug can discriminate between different receptors. Low specificity can cause side effects as it causes responses to multiple receptors

21
Q

scatchard plot

A

We use a scatchard plot to find the Kd specificity

22
Q

KI

A

KI value is used to characterise the ability to inhibit agonist binding to the receptor

23
Q

GPCRS

A

G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes

24
Q

Structure of GPCRS

A

There are Kinks in TM5-7 allowing for the conformational change
The largest conformational change in TM6 moving outwards from the central TM3 BY 14A
The small P(288 and 211) are proline residue they are hydrophobic residue and cause them to bend at these sites

25
Q

Ligands

A

Ligands bind to GDPR
Ligands include light-sensitive compounds, odors, pheromones, hormones and neurotransmitters
Lgands usually bind to extracellular sides

25
Q

Ligands

A

Ligands bind to GDPR
Ligands include light-sensitive compounds, odors, pheromones, hormones and neurotransmitters
Lgands usually bind to extracellular sides

26
Q

Forces in ligands

A

Ionic
Hydrogen
Hydrophobic
Steric factors

27
Q

Receptor signal transduction

A

Agonist bind to receptor

Receptor conformational change via TM5,6,7

28
Q

GPCR signalling

A

G proteins relay signal from GPCR to secondary messengers

29
Q

G protein subunits

A

Alpha-Main role in activating effectors
Beta
Gamma

30
Q

Ga protein signalling

A

Ga activates cAMP
cAMP then activates PKA
PKA phosphorylates other substances

31
Q

GPCR desensitisation

A

When a receptor is constantly bound to by a agonist causing response to be lower overtime

32
Q

Homologous desensitisation

A

desensitisation caused by phosphorylation of GPCR via PKA

Receptors and ion channels (8 decks)

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