Term
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Definition
| absorbtion, distribution, elimniation |
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Term
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Definition
| microenvironment of receptor |
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Term
| Receptor types and speeds |
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Definition
1. Ion channel - fastest
2. Enzyme dimers - 2nd slowest
3. G-protein
4. Steroid Hormone - slowest and in cytoplasm |
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Term
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Definition
=1/affinity = (d)(r)/(dr)
= concentration @ 50% receptors occupied |
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Term
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Definition
ability agonist to impart stimulus from binding receptor
either FULL or PARTIAL AGONIST |
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Term
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Definition
Non-linear response to receptor occupancy
*not 100% receptors need to be bound in order to elicit a maximum response* |
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Term
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Definition
| Dose at which 50% of maximal effect is elicited |
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Term
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Definition
| concentration required to produce required effect (IE affinity) |
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Term
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Definition
| Maximum stimulus a drug can impart |
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Term
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Definition
Can be replaced/compensated for with higher doses of agonist... shift dose response curve right
also called competitive |
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Term
|
Definition
| can actually antagonize full agonists!! |
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Term
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Definition
bind functional groups
cannot be overcome by agonist
think warfarin, aspirin, clopidogrel |
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Term
| constituatively active receptor |
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Definition
does not need a ligand to assume active conformation
bound by inverse agonist!! |
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Term
| drug that occupies only one receptor type |
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Definition
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|
Term
| drug that occupies multiple receptor types but only produces one type of effect at one concentration |
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Definition
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Term
|
Definition
| LD50/ED50 (always greater than one) |
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