Tacrine: Difference between revisions
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* Date of FDA Approval (Patent Expiration): 1993 (N/A)<br /> | * Date of FDA Approval (Patent Expiration): 1993 (N/A)<br /> | ||
* 1994 Sales: $100 Million | * 1994 Sales: $100 Million | ||
* | * Importance: One of the the first treatments for the symptoms of [[Alzheimer's Disease]], although no definitive proof exists as to whether it alters the progression of the disease. | ||
* | * See: [[Pharmaceutical Drugs]] for more information about other drugs and disorders | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
Tacrine is an [[Acetylcholinesterase]] (AChE) inhibitor. It binds to the active site of <scene name='Tacrine/Ache/1'>AChE</scene>, utilizing many of the same residues which <scene name='Tacrine/Ac/1'>bind and break down acetylcholine</scene>. By inhibiting AChE, the important neurotransmitter, acetylcholine, is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in [[Alzheimer's Disease]] patients. Tacrine <scene name='Tacrine/Bound/2'>primarily interacts with residues</scene> Phe 330, His 440, Trp 84, & Ser 200 in tightly binding to the AChE binding site via pi stacking interactions. It is clearly visible how <scene name='Tacrine/Inter/3'>Tacrine interferes</scene> with the binding of acetylcholine, outcompeting acetylcholine for nearly the same space in the active site. <ref>PMID:8415649</ref> | Tacrine is an [[Acetylcholinesterase]] (AChE) inhibitor. It binds to the active site of <scene name='Tacrine/Ache/1'>AChE</scene>, utilizing many of the same residues which <scene name='Tacrine/Ac/1'>bind and break down acetylcholine</scene>. By inhibiting AChE, the important neurotransmitter, [[acetylcholine]], is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in [[Alzheimer's Disease]] patients. Tacrine <scene name='Tacrine/Bound/2'>primarily interacts with residues</scene> Phe 330, His 440, Trp 84, & Ser 200 in tightly binding to the AChE binding site via pi stacking interactions. It is clearly visible how <scene name='Tacrine/Inter/3'>Tacrine interferes</scene> with the binding of acetylcholine, outcompeting acetylcholine for nearly the same space in the active site. <ref>PMID:8415649</ref> | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:Acetylcholinesterase Inhibitor Pharmacokinetics}} | |||
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===References=== | ===References=== | ||
