ACh transmission modulators

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8 Terms

1
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Nicotine

  • agonist

  • binds to neuronal nAChR, activating it

    • releases dopamine

  • similar structure to ACh

<ul><li><p>agonist</p></li><li><p>binds to neuronal nAChR, activating it</p><ul><li><p>releases dopamine</p></li></ul></li><li><p>similar structure to ACh</p></li></ul><p></p>
2
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chantix (varenicline)

  • partial agonist: competitive modulator

    • binds more tightly to nAChR than nicotine but does not cause receptor to open as much

  • partial mimicry of ACh structure: ring system instead

<ul><li><p>partial agonist: competitive modulator</p><ul><li><p>binds more tightly to nAChR than nicotine but does not cause receptor to open as much</p></li></ul></li><li><p>partial mimicry of ACh structure: ring system instead</p></li></ul><p></p>
3
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Conotoxin (snail venom)

  • antagonist, binds to muscle nAChR

  • prevents channel from open (cys loop pushed out)

    • no muscle activation

  • structure: surface is rigid and structured

<ul><li><p>antagonist, binds to muscle nAChR</p></li><li><p>prevents channel from open (cys loop pushed out)</p><ul><li><p>no muscle activation</p></li></ul></li><li><p>structure: surface is rigid and structured</p></li></ul><p></p>
4
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galantamine

  • noncompetitive inhibitor, binds to allosteric sites on nAChRs in prescence/absence of ACh

    • decreases activation of the nAChR

  • competitive reversible inhibitor of acetylcholinesterase (AChE)

    • binding prevents hydrolysis of ACh in neurons

    • slows cognitive decline in AD patients

<ul><li><p><strong>noncompetitive inhibitor,</strong> binds to <strong>allosteric</strong> sites on nAChRs in prescence/absence of ACh</p><ul><li><p>decreases activation of the nAChR</p></li></ul></li><li><p><strong>competitive reversible inhibitor</strong> of <strong>acetylcholinesterase</strong> (AChE)</p><ul><li><p>binding prevents hydrolysis of ACh in neurons</p></li><li><p>slows cognitive decline in AD patients</p></li></ul></li></ul><p></p>
5
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hemicholinium

  • mimics Choline, binds in cleft of choline transporter but too large to pass through

    • slows ACh synthesis

    • can offset ACh accumulation by VX

<ul><li><p><strong>mimics Choline</strong>, binds in cleft of<strong> choline transporter </strong>but too large to pass through</p><ul><li><p>slows ACh synthesis</p></li><li><p>can offset ACh accumulation by VX</p></li></ul></li></ul><p></p>
6
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VX Gas

  • irreversibly inhibits AChE: its phosphonate not hydrolyzed; highly reactive

    • active site serine of AChE attacks phosphorus instead of breaking down ACh using the Ser-His-Glu triad

<ul><li><p>irreversibly inhibits AChE: its phosphonate not hydrolyzed; highly reactive </p><ul><li><p>active site serine of AChE attacks phosphorus instead of breaking down ACh using the Ser-His-Glu triad</p></li></ul></li></ul><p></p>
7
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Botox

  • heavy chain binds to synaptotagmin

    • gets imported with recycled empty vesicles

  • light chain released into cytosol

    • cleaves SNARE proteins

    • ACh release into synaptic cleft inhibited

    • no muscle contraction

<ul><li><p>heavy chain binds to synaptotagmin</p><ul><li><p>gets imported with recycled empty vesicles</p></li></ul></li><li><p>light chain released into cytosol</p><ul><li><p>cleaves SNARE proteins</p></li><li><p>ACh release into synaptic cleft inhibited</p></li><li><p>no muscle contraction</p></li></ul></li></ul><p></p>
8
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epibatidine

  • agonist of ACh

  • very high binding affinity, very potent

  • blocks pain receptors without being an opioid but very toxic

<ul><li><p>agonist of ACh</p></li><li><p>very high binding affinity, very potent</p></li><li><p>blocks pain receptors without being an opioid but very toxic</p></li></ul><p></p>