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Constriction

Parasympathetic

• Pupils

Decreased heart rate

Parasympathetic

• Heart

Broncho constriciton

Parasympathetic

• Lungs

Stimulates digestion

Parasympathetic

• Stomach

Glycogen storage

Parasympathetic

• Liver

Sexual arousal

Parasympathetic

• Reproduction

Contraction

Parasympathetic

• Bladder

Dilation

Sympathetic

• Pupils

Accelerates cardiac rhythm

Sympathetic

• Heart

Increased airflow (broncodilation)

Sympathetic

• Lungs

Inhibits digestion

Sympathetic

• Stomach

Promotes glycogenolysis

Sympathetic

• Liver

Inhibits sexual functions

Sympathetic

• Reproduction

Relaxation

Sympathetic

• Bladder

Brain

• Cerebrum

• Brainstem

• Cerebellum

Brainstem

• Midbrain

• Pons

• Medulla

Spinal cord

Central nervous system

• Parts of a brain

• Acetylcholine

• Norepinephrine

• Dopamine

• Serotonin

Important neurotransmitters

• a1

• a2

• b1

• b2

Adrenergic Receptors

• Nicotinic receptors

• Muscarinic receptors

Cholinergic receptors

Acetylcholine

Natural neurotransmitter of Cholinergic system

• Bethanechol

• Pilocarpine

Cholinergic agonists

• Neostigmine

• Physostigmine

Acetylcholinesterase inhibitors

• Enzyme inhibition

• Carbamate functional group

Acetylcholinesterase inhibitors key concepts

• Atropine

• Scopolamine

Anticholinergic drugs

• Tertiary amine vs quaternary amine

• Lipid solubility and CNS penetration

Focus of anticholinergic drugs

• Norepinephrine

• Epinephrine

Neurotransmitters of the Adrenergic System

Alpha (1,2)

Beta (1,2,3)

Adrenergic System Receptors

• Epinephrine

• Phenylephrine

• Salbutamol

Adrenergic agonists

• Catechol ring

• Hydroxyl substitution

• Amine side chain modification

Medicinal chemistry focus on adrenergic agonists

• Propranolol

• Prazosin

Adrenergic antagonists

• Aryloxypropanolamine structure

• Selectivity of beta blockers

Key SAR of Adrenergic antagonists

• Serotonin

• Dopamine

• Noradrenaline

• GABA

• Acetylcholine

• Glutamic acid

Hormones and mood neurotransmitters

• Lipophilicity

• Molecular size

• Degree of ionization

• Hydrogen bonding

Blood brain barrier

• Important factors affecting drug penetration

• Sedatives and Hypnotics

• Antidepressants

• Antipsychotics

• Anticonvulsants

Major CNS drug classes

• Diazepam

• Phenobarbital

Sedatives and hypnotics

• Fluoxetine

• Amitriptyline

Antidepressants

• Chlorpromazine

• Haloperidol

Antipsychotics

• Phenytoin

• Valproic acid

Anticonvulsants

• Benzodiazepine ring system

• Barbituric acid derivatives

• Interaction with GABA receptors

Medicinal chemistry topics regarding sedatives and hypnotics

• Tricyclic structure

• Serotonin reuptake inhibition

• Lipophilic aromatic rings

Topics under antidepressants

• Dopamine receptor antagonism

• Phenothiazine scaffold

Focus of antipsychotics

• Hydantoin ring

• Sodium channel inhibition

• SAR

Medicinal chemistry of anticonvulsants