Chemical Transmission and Receptors Flashcards

1
Q

Describe ionotropic receptors

A

Specific ligand activated
Directly alter ionic currents
Rapid response
Doesn’t amplify the signal

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2
Q

Describe metabotropic receptors

A

Indirectly alters ionic currents
Slower response
Amplify the signal

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3
Q

Describe receptor tyrosine kinases

A

Indirectly alters ionic currents by phosphorylating 2nd messengers or the receptor directly
Slower response
Amplify the signal

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4
Q

Describe G-protein coupled receptors (GPCRs)

A

Consists of 7 membrane spanning alpha helices

Guanin nucleotide-binding proteins termed G proteins

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5
Q

State the three subunits of GPCRs

A

Alpha
Beta
Gamma

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6
Q

Describe the resting state of GPCRs

A

Resting inactive state= GDP is bound to a subunit

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7
Q

Describe the ligand binding step of activation of GPCRs

Explain influence of GEFs and GAP

A

Ligand binding promotes a conformational change in heterotrimer and release of GDP and binding of GTP

Guanine exchange factor (GEFs) facilitates this exchange

GTPase (GTPase activating protein, GAP) is associated with g protein activation but cleavage to GDP leads to inactivation

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8
Q

Describe the stimulation step of GPCRs

A

GDP-GTP exchange stimulates dissociation of G Protein complex from receptor

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9
Q

GAP proteins involved in GPCRs

A

Regulation of G-protein signalling

Family of proteins that enhance some alpha subunits and GTPases activity

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10
Q

State properties of alpha and betagamma effector molecules

A

Alpha= water soluble

Betagamma= lipid associated

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