Essential Pharmacology Flashcards

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1
Q

Basic functions of receptors

A

They can detect changes in the environment, stimuli, and turn them into electrical signals and enable an appropriate response.
Intracellular receptors; live inside the cell so can only be activated by lipophilic compounds eg steroid hormones, NO. Used for transcription and cell activity.
Plasma membrane receptors/ionotropic receptors; fast EPSPs/IPSPs. Used for intrinsic enzyme activity, proliferation, differentiation and JAK kinase-protein synthesis.
G-proteins; coupled to phosphilipase C - activates Protein kinase C, releases Ca2+. Coupled to adenyl cyclase increases/decreases cAMP and activates protein kinase A. Coupled to ion channels gives rise to slow EPSPs/IPSPs

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2
Q

Receptor

A

They are transducers (convert physical quantity to electrical signal) that convert different forms of energy into frequency of APs. They turn a signal into a response.

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3
Q

Agonist

A

A substance which initiates a physiological response when combined with a receptor. Mimics normal action.

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4
Q

Antagonist

A

A substance that blocks or dampens a biological response by binding to and blocking a receptor. Blocks normal action.

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5
Q

Ec50

A

The effective concentration producing 50% of the maximum response. A low Ec50 equals a high affinity.

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6
Q

Affinity

A

Affinuty is determined by the strength of chemical attraction between drug and receptor.
Full agonist has a high affinity and efficacy so fully activates the receptor.
Partial agonist has a high affinity and medium efficacy so partially activates.
An antagonist has a high affinity but low efficiacy so there is no activation.

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7
Q

Efficacy

A

Efficacy is determined by how good the drug is at activating the receptor.

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8
Q

Describe the transmission of transmembrane signalling

A

An extracellular signal acts on a receptor causimg an intracellular signal and activation of effector.

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9
Q

Sources of intracellular Ca2+

A
  1. Via inositol trisphosphate (IP3)
  2. Via stimulated release of Ca2+ from endoplasmic reticulum
  3. Extracellular via v.gated or L.gated Ca2+ channels.
  4. Inhibition of Ca2+ transport out of cell
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