Term
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Definition
| AChE - an enzyme breaks down acetylcholine into choline and acetate |
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Term
| acetylcholinesterase's structural classes |
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Definition
1. Alcohol with quat
2. Carbamic Acid Esters
3. Organophosphates |
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Term
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Definition
rapid, reversible bloc bc non-covalent drug-enz bond
e.g. Edrophonium |
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Term
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Definition
-longer inhibition
-labile covalent bond after HOH and AChE
-quat and tert amines use
e.g. Neostigmine (quat), Physostigmine (tert) |
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Term
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Definition
-irrev inhibition
-very stable complex after HOH and aging
e.g. nerve gas, insectisized usages
e.g. Isoflurophate, pralidoxime |
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Term
| muscarinic receptor agonists's structural classes |
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Definition
1. Choline Esters
2. Alkaloids |
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Term
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Definition
-ACh aka aminoalc ester
-All quats
-Little CNS penetration
-Poor oral absorp
e.g. Acetylcholine, Methachline, Carbachol, Bethaechol |
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Term
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Definition
-Atropine & Scopolamine (both alkaloids and tert)
-Ipratropium (Atrovent)
-Tiotropium (Spirivia) |
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Term
|
Definition
-Glycopyrrolate
-Oxybutynin |
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Term
| muscarinic receptor antagonists |
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Definition
*All are aminoacohol esters:
-Tropanes (most common is Atropine)
-Non-Tropanes
(also see Foye fig 12.19)
*synthetic agent (circle's structure of Atropine)
-Anticholinergics Aminoalcohols (e.g. Tolterodine -amine)
-Anticholinergics Aminoethers (Benzotropine, Cogentin-for Parkinson)
-Misc Anticholinergics
. Propantheline
. Solifinacin
. Darifenacin |
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Term
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Definition
| structure-activity relationship |
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Term
|
Definition
| absorption, distribution, metabolism, and excretion |
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Term
| nicotinic receptor antagonists |
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Definition
-Ganglionic Blockers
-Neuromuscular Blockers (NMJ Blockers) |
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Term
|
Definition
-Trimethaphan & Mecamylamine
-Hexamethonium SAR |
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Term
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Definition
-Curare & Steroid-base (Pancuronium, vacuronium, pipecuronium, rocuronium)
-Succinylcholine & Decamethonium SAR |
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Term
|
Definition
-Do not cross membrane barriers
-GI, BBB absorption impaired
-Typically no CNS effect |
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Term
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Definition
-Good CNS penetration
e.g. Physostigmine-agent of choice to tx CNS effects of anticholinergic overdose (e.g. tubocurare poisoning) |
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Term
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Definition
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Term
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Definition
| Lambert Eaton Myasthenic Syndrome: (NMJ disease) autoimmune disorder that affects (blocked) voltage gated channel -> less transmitter released -> no contraction due to inhibition of vescicle fusing at presynaptic |
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Term
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Definition
| Transport ACh into vesicle (requires transport ATP energy) |
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Term
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Definition
| an esperimental drug acting presynaptically inhibiting ACh (against ACh storage) |
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Term
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Definition
| a drug which blocks the reuptake of choline |
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Term
| video of action of mAChR M1,M2,M3 |
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Definition
| http://www.bio.davidson.edu/courses/immunology/Flash/IP3.html |
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Term
|
Definition
| Phospholipase C, an ezyme cleaves phospholipid to produce IP3 and DAG; consequently produce Ca++ and PKC |
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Term
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Definition
| excitatory postsynaptic potential (EPSP) is a graded depolarization of a postsynaptic membrane in response to stimulation by a neurotransmitter |
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Term
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Definition
| end plate potentials are the depolarizations of the skeleton muscle fibers caused by neurotransmitters binding to the postsynaptic membrane in the NMJ |
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Term
| mechanism of ionotropic receptor (e.g. nAChR) or ligand-gated ion channel (LGIC) |
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Definition
| When activated, it opens a channel that allows ions such as Na+, K+, or Cl- to flow |
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Term
| mechanism of G protein-linked receptor (e.g. mAChR) |
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Definition
| Gq/11 mechanism (EPSP) or Beta Gamma of G protein |
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Term
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Definition
| PLC->increase IP3 and increase DAG -> increase Ca++ and increase PKC (e.g. M1, M3, M5 - excitatory) |
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Term
| Beta Gamma of G protein mechanism |
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Definition
| inhibit AC and increase K+ channel opening (e.g. M2, M4 - inhibitatory) |
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