What is Arecoline?
A natural alkaloid found in the betel nut, acting as a muscarinic agonist.
What are parasympathomimetic drugs?
Drugs that mimic the effects of the parasympathetic nervous system.
p.14
Structure-Activity Relationship (SAR) for Acetylcholine
What is an acyloxy group?
A functional group derived from an acid by replacing the hydroxyl group with an alkoxy group.
p.22
Structure-Activity Relationship (SAR) for Acetylcholine
What effect does a b-methyl group have on muscarinic potency?
It increases muscarinic potency and selectivity.
p.29
Muscarinic Receptors (M1-M5)
What is a binding site in the context of muscarinic receptors?
A specific location on the muscarinic receptor where acetylcholine or other ligands can attach.
p.28
Muscarinic Receptors (M1-M5)
What role do binding sites play in muscarinic receptors?
They facilitate the interaction between the receptor and neurotransmitters, leading to a physiological response.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
What role does the acetyl group play in acetylcholine's structure?
It is essential for the molecule's stability and receptor interaction.
Name a choline ester that acts as a cholinergic agonist.
Acetylcholine or Bethanecol.
p.15
Structure-Activity Relationship (SAR) for Acetylcholine
What does the term 'Synperiplanar' refer to?
A configuration where substituents are on the same side of a reference plane.
What is Xanomeline?
A selective muscarinic agonist used in research and potential treatment for Alzheimer's disease.
p.28
Muscarinic Receptors (M1-M5)
How do muscarinic binding sites affect cellular signaling?
They initiate a cascade of intracellular events upon ligand binding, influencing various physiological functions.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
What effect does the modification of the ethylene bridge in acetylcholine have?
It can alter the potency and selectivity for cholinergic receptors.
What are cholinergic agonists?
Substances that stimulate the cholinergic receptors in the body.
What is the primary action of cholinergic agonists?
They mimic the action of acetylcholine.
p.16
Pharmacological Applications of Cholinergic Drugs
What is a potential side effect of cholinergic agonists?
Increased salivation and sweating.
What type of activity does the potent cholinergic agonist possess?
Both muscarinic and nicotinic activity.
p.15
Structure-Activity Relationship (SAR) for Acetylcholine
What is a 'Synclinal' structure?
A geological fold that is concave upward, with the youngest rocks at the center.
p.29
Muscarinic Receptors (M1-M5)
What type of molecules typically bind to muscarinic receptors?
Acetylcholine and other muscarinic agonists.
p.27
Structure-Activity Relationship (SAR) for Acetylcholine
What does SAR stand for in the context of muscarinic agonists?
Structure-Activity Relationship.
p.44
Structure-Activity Relationship (SAR) for Acetylcholine
What is the stereochemistry of Pilocarpine?
3 S, 4 R -(+)-pilocarpine.
p.26
Structure-Activity Relationship (SAR) for Acetylcholine
How does the size of the alkyl groups in acetylcholine influence its activity?
Larger alkyl groups can reduce receptor affinity and alter pharmacological effects.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
What is the significance of the quaternary ammonium in acetylcholine?
It enhances the molecule's solubility and interaction with receptors.
p.29
Muscarinic Receptors (M1-M5)
What role do binding sites play in muscarinic receptors?
They facilitate the interaction between the receptor and neurotransmitters, leading to a physiological response.
p.42
Pharmacological Applications of Cholinergic Drugs
What happened to the production in Taiwan according to the article?
Production was halted due to the herb's effects.
p.42
Pharmacological Applications of Cholinergic Drugs
What is the significance of the herb mentioned in the article?
It has a notable impact on the production process.
What are direct acting cholinergic agonists?
They act on the receptors to activate a tissue response.
p.33
Hydrolysis of Acetylcholine by Acetylcholinesterase
What is the significance of Trp 86 in AChE?
It is part of the esteratic site.
p.28
Muscarinic Receptors (M1-M5)
What is a binding site in the context of muscarinic receptors?
A specific location on the muscarinic receptor where acetylcholine or other ligands can attach.
p.15
Structure-Activity Relationship (SAR) for Acetylcholine
Define 'Anticlinal'.
A geological fold that is convex upward, with the oldest rocks at the center.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
What is the primary function of acetylcholine in the body?
It acts as a neurotransmitter in the nervous system.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
What is the primary function of acetylcholine in the body?
It acts as a neurotransmitter in the nervous system.
p.11
Muscarinic Receptors (M1-M5)
Where are muscarinic receptors found?
In smooth muscles and cardiac muscles.
p.19
Direct and Indirect Acting Cholinergic Agonists
What are the two types of cholinergic agonists?
Direct-acting and indirect-acting cholinergic agonists.
List some carbamate cholinesterase inhibitors.
Physostigmine, Neostigmine, Pyridostigmine, Edrophonium.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
How does the structure of acetylcholine influence its activity?
The presence of an ester group and a quaternary ammonium group are crucial for its binding to receptors.
p.22
Structure-Activity Relationship (SAR) for Acetylcholine
How much more potent is S-(+) compared to R-(-) in terms of muscarinic activity?
S-(+) is 20-fold more potent than R-(-).
p.44
Pharmacological Applications of Cholinergic Drugs
What type of reaction is base-catalyzed epimerization?
A reaction that involves the conversion of one epimer to another, typically under basic conditions.
p.43
Pharmacological Applications of Cholinergic Drugs
What are the forms in which pilocarpine is available?
Tablets, ophthalmic solution, and gel.
p.26
Structure-Activity Relationship (SAR) for Acetylcholine
What is the significance of SAR in relation to acetylcholine?
It helps in understanding how the structure of acetylcholine affects its activity and interactions with receptors.
What is Oxotremorine?
A synthetic muscarinic agonist that is used in research to study cholinergic systems.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
How does the structure of acetylcholine influence its activity?
The presence of an ester group and a quaternary ammonium group are crucial for its binding to receptors.
p.27
Structure-Activity Relationship (SAR) for Acetylcholine
What is a common feature of muscarinic agonists in terms of structure?
They often contain an ester group.
p.27
Structure-Activity Relationship (SAR) for Acetylcholine
What role do nitrogen atoms play in muscarinic agonists?
They are crucial for binding to the receptor.
p.19
Major Uses of Cholinergic Agonists
Name a common use of cholinergic agonists.
They are often used to treat conditions like glaucoma and myasthenia gravis.
p.16
Pharmacological Applications of Cholinergic Drugs
How do cholinergic agonists affect smooth muscle?
They stimulate contraction of smooth muscle.
What is the anticholinesterase activity level of this cholinergic agonist?
Weak anticholinesterase activity.
p.15
Structure-Activity Relationship (SAR) for Acetylcholine
What does 'Antiperiplanar' mean?
A configuration where substituents are on opposite sides of a reference plane.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
What does SAR stand for in the context of acetylcholine?
Structure-Activity Relationship.
p.11
Nicotinic Receptors (N1 & N2)
What are the two types of nicotinic receptors?
Neuronal (N1) and Muscle (N2).
p.19
Direct and Indirect Acting Cholinergic Agonists
What is the role of indirect-acting cholinergic agonists?
They inhibit acetylcholinesterase, increasing acetylcholine levels.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
What is the primary function of acetylcholine in the body?
It acts as a neurotransmitter in the nervous system.
What does 'equipotent' mean in the context of S -(+) and Ach?
It means that S -(+) has the same potency as Acetylcholine.
p.14
Structure-Activity Relationship (SAR) for Acetylcholine
What does the number 19 refer to in this context?
It is unclear without additional context; it may refer to a specific compound or classification.
p.44
Pharmacological Applications of Cholinergic Drugs
What role does CYP2A6 play in relation to Pilocarpine?
It acts as a CYP2A6 inhibitor.
p.27
Structure-Activity Relationship (SAR) for Acetylcholine
How does the presence of a bulky group affect muscarinic agonists?
It can enhance selectivity for muscarinic receptors over nicotinic receptors.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
What modifications can affect the activity of acetylcholine?
Changes to the ester or ammonium groups can alter receptor binding and enzymatic hydrolysis.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
What is the significance of the ethylene bridge in acetylcholine?
It helps maintain the spatial arrangement necessary for receptor interaction.
p.14
Structure-Activity Relationship (SAR) for Acetylcholine
What is an ethylene group?
A hydrocarbon group consisting of two carbon atoms connected by a double bond.
p.26
Structure-Activity Relationship (SAR) for Acetylcholine
What does SAR stand for in the context of acetylcholine?
Structure-Activity Relationship.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
What does SAR stand for in the context of acetylcholine?
Structure-Activity Relationship.
p.26
Structure-Activity Relationship (SAR) for Acetylcholine
How does the presence of a quaternary ammonium group affect acetylcholine's activity?
It enhances its binding affinity to cholinergic receptors.
p.26
Structure-Activity Relationship (SAR) for Acetylcholine
What role does the ester group play in acetylcholine's structure?
It is crucial for the hydrolysis of acetylcholine by acetylcholinesterase.
p.33
Hydrolysis of Acetylcholine by Acetylcholinesterase
What is the role of Acetylcholinesterase (AChE) in the hydrolysis of acetylcholine?
AChE catalyzes the breakdown of acetylcholine into acetate and choline.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
What is the significance of the quaternary ammonium in acetylcholine?
It enhances the molecule's solubility and ability to interact with cholinergic receptors.
p.35
Major Uses of Cholinergic Agonists
What are the major uses of cholinergic agonists?
Stimulate bladder and GI tone, constrict pupils, and enhance neuro-muscular transmission.
Which routes of administration should be avoided to minimize systemic cholinergic effects?
IV (intravenous) or IM (intramuscular).
p.14
Structure-Activity Relationship (SAR) for Acetylcholine
What is a quaternary ammonium group?
A positively charged nitrogen atom bonded to four organic groups.
p.44
Pilocarpine and Cevimeline
What is Pilocarpine known for?
It is a more stable carbamate compound.
p.42
Pharmacological Applications of Cholinergic Drugs
What is the main topic of the article?
The article discusses the impact of a certain herb on the production of a specific product in Taiwan.
p.27
Structure-Activity Relationship (SAR) for Acetylcholine
What is the significance of SAR in muscarinic agonists?
It helps to understand how structural changes affect the activity of the agonists.
p.21
Structure-Activity Relationship (SAR) for Acetylcholine
What role does the acetyl group play in acetylcholine's structure?
It is important for the molecule's stability and receptor interaction.
What are cholinergic agonists?
Substances that stimulate the cholinergic receptors in the body.
p.16
Pharmacological Applications of Cholinergic Drugs
What is the effect of cholinergic agonists on the heart?
They generally decrease heart rate.
p.23
Structure-Activity Relationship (SAR) for Acetylcholine
How does the structure of acetylcholine influence its activity?
The presence of an ester group and a quaternary ammonium group are crucial for its binding to receptors.
p.33
Hydrolysis of Acetylcholine by Acetylcholinesterase
What is the function of the anionic site in AChE?
It helps in the binding of acetylcholine.
p.11
Muscarinic Receptors (M1-M5)
What is the effect of activating M4 receptors?
Inhibits acetylcholine release in the striatum.
Name a type of indirect acting cholinergic agonist.
Cholinesterase inhibitors.
What is the primary action of cholinergic agonists?
They mimic the action of acetylcholine.
p.16
Major Uses of Cholinergic Agonists
Name a common use of cholinergic agonists.
They are often used to treat conditions like glaucoma and myasthenia gravis.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
What happens if modifications are made to the acetylcholine structure?
Changes can affect its potency, selectivity, and duration of action.
What do indirect acting cholinergic agonists do?
They inhibit the action of the enzyme Acetylcholinesterase.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
What role does the acetyl group play in acetylcholine's structure?
It is important for the molecule's stability and receptor binding.
p.16
Direct and Indirect Acting Cholinergic Agonists
What are the two types of cholinergic agonists?
Direct-acting and indirect-acting cholinergic agonists.
p.24
Structure-Activity Relationship (SAR) for Acetylcholine
What does SAR stand for in the context of acetylcholine?
Structure-Activity Relationship.
