Term
| Properties of the Ideal Drug |
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Definition
Specific Action
Potent
Appropriate duration of action
Easy administration
Minimal side effects or toxicity in dosage range
Low cost |
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Term
| What are the targets for drug action? |
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Definition
| receptors, ion channels, enzymes, carrier molecules |
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Term
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Definition
| A receptor is a protein macromolecule either on or in a cell. They act as recognition sites for endogenous ligands. Ligands can be neurotransmitters, hormones, immunological mediators etc. |
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Term
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Definition
| An agonist binds to the same site as the endogenous ligand producing the same kind of signal. |
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Term
| A drug that binds to a receptor at a site distinct from the active site is called? |
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Definition
| An allosteric modulator. The modulator produces no signal itself but enhances the signal of the endogenous ligand. |
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Term
| what does a negative allosteric modulator do? |
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Definition
| It bind to an allosteric site on the receptor and diminishes the signal produced by the endogenous ligand. |
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Term
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Definition
| It is the tendency of the drug molecule to bind to the receptor. |
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Term
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Definition
| It is the tendency of the drug molecule to activate the receptor once bound. |
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Term
| what is bound to alpha subunit of G protein when it is inactive. |
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Definition
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Term
| Which loop of the GPRC is coupled to the G protein |
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Definition
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Term
| Name three examples of GPCR |
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Definition
1. Muscarinic ACh receptor
2. Adrenergic receptors
3. Dopamine receptors |
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Term
| What causes the alpha subunit to re-associate with the beta/gamma complex. |
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Definition
| The GTPase activity of the alpha sub-unit increases when it binds to the target protein. This leads to hydrolysis of the bound GTP to GDP whereupon the alpha sub-unit reunites with the beta/gamma complex |
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Term
| Name the four different G protein subtypes |
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Definition
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Term
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Definition
Gs stimulates adenylate cyclase which increases cAMP formation.
A typical effect is at the beta adrenergic receptor. Increased cAMP causes smooth muscle to relax. |
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Term
| Which G protein subtype inhibits Adenylate cyclase. |
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Definition
| Gi inhibits adenylate cyclase and thereby reduces cAMP formation. ACh binds to MAChR. Gi is expressed. Decreased cAMP decreases force of contraction of the heart. |
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Term
| Name the G protein sub types that inhibit specific inhibitors |
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Definition
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Term
| Name G protein subtypes that activate effectors |
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Definition
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Term
| Name the main targets for G proteins |
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Definition
1. Adenylate Cyclase
2. Phopholipase C
3. Rho A/Rho Kinase
4. Mitogen - activated protein kinase (MAP Kinase) |
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