Receptors Flashcards

1
Q

What does intrinsic activity mean?

A

The drug binds to the receptor but it doesn’t activate it.

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2
Q

What is the difference between a competitive and non-competitive antagonist?

A

Competitive - binds to the same receptor site as the agonist.
Non-competitive - binds to a different site

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3
Q

How can the effect of a competitive antagonist be overcome?

A

By increasing the concentration of agonist.

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4
Q

Emax is a measure of what?

A

Efficacy.

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5
Q

What is pA2?

A

The negative logarithm of the molar concentration of antagonist that produces an agonist does ratio of 2.

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6
Q

What is the primary inhibitory neurotransmitter in the CNS?

A

GABA

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7
Q

What type of receptor is the GABAa receptor?

A

Ligand-gated ion channel receptor.

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8
Q

What are benzodiazepines used for?

A

Treating anxiety, e.g. diazepam.

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9
Q

How do benzodiazepines increase the inhibitory effect of GABA?

A
  1. By increasing the affinity of the receptor for GABA

2. The frequency of ion channel opening

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10
Q

What is receptor supersensitivity?

A

Increase in receptor number.

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11
Q

What is responsible for myelinating axons in the CNS?

A

Oligodendrocytes

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12
Q

What is a neuromuscular junction?

A

A synaptic connection between a motor nerve and skeletal muscle.

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13
Q

What are the receptors for acetylcholine?

A

Nicotinic acetylcholine receptors (ligand-gated ion channel receptors)

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14
Q

Noradrenaline is released from every post-ganglion in nerve fibre except for?

A

The sweat glands - they release adrenaline.

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15
Q

Which receptors are activated to cause pupil constriction in the eye as a parasympathetic response?

A

M3 muscarinic receptors

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16
Q

What is the sympathetic response for the heart and which receptors are involved?

A

Increased heart rate and force of contraction, b1 adrenergic receptors

17
Q

What is the sympathetic response for the GI tract?

A

Decreased motility (b2 adrenergic) and sphincter constriction (a1)

18
Q

Name the a1-adrenergic antagonists.

A

Prazosin, doxazosin