504 Pharm: Princ Of Drug Actions I

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504 PHARM: PRINC OF DRUG ACTIONS I

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504 PHARM: PRINC OF DRUG ACTIONS I

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Drug

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A molecule that modifies physiological function.

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Types of receptors?

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1. G protein coupled receptors
2. ligand-gated ion channels
3. steroid receptors
4. growth factor receptors

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G Protein Coupled Receptors

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1. On cell surface
2. Activated by NTs and hormones.
3. Act by associating with G proteins inside cell

NOTE: cell surface receptors have one part of receptor contacting extracellular space while another contacting intracellular space.

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Ligand-gated ion channels

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1. on cell surface
2. activated by NTs
3. act by opening pores to allow ions to pass thru.

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Steroid receptors

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1. inside cell
2. activated by steroids and other molecules.
3. act by altering gene transcription.

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Growth factor receptors

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1. on cell surface
2. activated by GFs
3. these receptors are enzymes that catalyze phosphorylation rxn inside cell.

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How are receptors classified?

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Classified into families based on endogenous compound that bind to and activate them.

ex: adrenergic receptors: adrenaline (epi)

cholinergic receptors: Ach

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Subtypes of adrenergic and cholinergic receptors:

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Adrenergic subtypes:
1. alpha, then alpha 1, alpha 2
2. beta, then beta 1, beta 2

Cholinergic subtypes:
1. nicotinic
2. muscarinic

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Beta 1

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Adrenergic receptors of cardiac cells

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Beta 2

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Adrenergic receptors of smooth muscle cells

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Agonist

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Binds to and activates receptor

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Antagonist

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Binds to, but does not activate. Prevents agonist from binding.

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Modulator

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Binds to receptor at a site distinct from where AGONISTS bind and modulates receptor function.

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Drug affinity eqtn:

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Kd = [free drug] [unbound receptor]/ [drug-receptor complex]

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Receptor ANTAGONISTS often have what affinity for their receptor?

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HIGH

and receptor agonists have LOW affinity for their receptors.