Chemistry of recoptor binding, modulators, agonist and antagonists
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| Most receptors are located in... | the cell membrane
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| Receptors are activated by... | Chemical messengers
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| Chemical messengers include _____ and ______ | neurotransmitters and hormones
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| Binding of messenger to receptor results in _______ _______ | Signal transduction
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| Drug that mimics natural messenger is an _____ | agonist
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| Agonist should bind and leave quickly or slowly? | quickly
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| Drug that blocks natural messenger is an _____ | antagonist
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| Antagonists alter induced fit due to _____ and/or _____ binding groups | stronger and/or more binding groups
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| Agonist must have correct ____ , ______ and ____ _____ in order to work | correct shape , positioning and binding groups
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| Enantiomers usually have ______ biological properties | different
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| Agonists usually have _____ of interactions as natural messenger | same #
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| Groups that block access to binding site are called ______ or ______ | steric blocks or steric shields
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| Agents which bind to allosteric binding site rather than the messenger binding site | allosteric modulators
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| Allosteric modulators _______ receptor activity | enhance
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| Ex. of Allosteric modulator | benzodiazepines
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| Benzodiazepines target allosteric site of | GABAa receptor
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| Reversible antagonist binds _____ to receptor and produces different ____ ___ | reversibly , induced fit
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| Does antagonist undergo rxn with receptor? | no rxn
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| Level of antagonism depends on _____ of binding and _______ | strength and [antagonist]
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| For reversible antagonist: increasing [messenger].... | lowers antagonism
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| Irreversible antagonists bind _____ to receptor by form ______ bonds | irreversibly , covalent
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| For irreversible antagonists: increasing [messenger]... | does not reverse antagonism
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| Allosteric antagonist bind ______ to _______ site of receptor | reversibly , allosteric
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| Alloseric antagonist work by.... | altering shape of receptor to block messenger action
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| For Allosteric antagonists: increasing [messenger]... | does not reverse antagonism
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| How does Antagonism by Umbrella effect work? | Antagonist binds to neighboring binding site and overlaps/covers messenger binding site
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| ______ ______ binds but does not produce maximum effect | Partial agonist
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| Partial agonists act as _____ to one receptor subtype and ______ to different subtype | agonist , antagonist
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| Define Inherent activity | any activity present in the absence of a chemical messenger
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| Inverse agonist blocks ______ ______ of receptor | inherent activity
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| Inverse agonist create equilibrium between ______ activity and _______ | inherent activity and inactivity
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| Adding agonist pushed receptor toward _____ form | active
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| Adding antagonist pushes receptor toward ____ form | inactive
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| Adding partial agonist pushes receptor toward ______ between forms | equilibrium
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| Receptors become ____ after long-term exposure to agonist | desensitized
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| Prolonged binding of agonist leads to ______ of receptor | phosphorylation
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| Phosphorylation _______ receptor until agonist leaves | deactivates
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| Receptors become ______ after long-term exposure to antagonist | sensitized
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| To compensate for antagonist-blocked receptors, cell.... | synthesizes new receptors
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| Synthesis of new receptors makes cell more sensitive to _______ | natural messenger
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| Long-term exposure to agonist can lead to ______ and ______ | tolerance and dependence
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| Tolerance results in need to.... | increase dosage of antagonist
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| Dependence results from ______ symptoms when antagonist is taken away | withdrawal
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| Estradiol binding to estrogen receptor results in _______ and exposure of _____ | dimerization , AF-2 regions
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| _______ binds to AF-2 regions of estrogen receptor in order to activate response | Coactivator
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| Raloxifene is an estrogen receptor ______ and ______ agent | antagonist and anti-cancer
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| Raloxifene works by preventing ______ so _____ regions are not exposed and coactivator doesn't bind | dimerization , AF-2
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| Tamoxifen is an estrogen receptor ______ | antagonist
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