[MEDORG-SEMIS-02-PT2] OUTLINE OF SEMIS TOPIC

THIS FLASHCARDS IS ABOUT [MEDORD] OUTLINE OF CENTRAL NERVOUS SYSTEM.

Ligand-gated ion channel

What type of receptor is the nicotinic receptor?

Cell depolarization due to Na/K ion flow

What happens when nicotinic receptors are activated?

• M1

• M3

• M5

Which muscarinic receptors are coupled to Gq proteins (3)?

IP3/DAG cascade leading to PKC activation

What intracellular pathway is activated by Gq-coupled receptors?

M1

(Linked to adenylate cyclase)

Which muscarinic receptor is coupled to Gs protein?

• Increases adenylate cyclase

• Increases cAMP

• Activates PKA

What is the effect of Gs protein activation?

• M2

• M4

Which muscarinic receptors are coupled to Gi proteins?

• Decreases adenylate cyclase

• Decreases cAMP

What is the effect of Gi protein activation?

Acetylcholine

What neurotransmitter is released by all preganglionic autonomic neurons?

Nicotinic (Nn or N2) receptor

What receptor is found in autonomic ganglia?

Norepinephrine

What neurotransmitter is released by most postganglionic sympathetic neurons?

Adrenergic receptors (alpha and beta)

What receptor does norepinephrine act on in target organs?

Sweat glands use ACh (not norepinephrine).

What is the sympathetic exception involving sweat glands?

Epinephrine (and some norepinephrine)

What does the adrenal medulla release into the bloodstream?

Muscarinic receptor

What receptor is found at the effector organ in the parasympathetic division?

Acetylcholine

In cholinergic system (parasympathetic), what is the natural neurotransmitter?

• Muscarinic

• Nicotinic

What are the (2) Receptors in Cholinergic System (Parasympathetic)?

• Cholinergic Agonists

• Acetylcholinesterase Inhibitors

• Anticholinergic Drugs

What are the (3) drug categories of Cholinergic System (Parasympathetic)?

• Bethanechol

• Pilocarpine

What are the (2) Examples of Cholinergic Agonists?

Hint: Black Pink

• Ester stability

• Quaternary ammonium group

• SAR of choline esters

• Neostigmine

• Physostigmine

What are the (2) Examples of Acetylcholinesterase Inhibitors?

Hint: No Problem

• Enzyme inhibition

• Carbamate functional group

• Atropine

• Scopolamine

What are the (2) Examples of Anticholinergic Drugs?

Hint: ATRO-SCO

• Tertiary amine vs quaternary amine

• Lipid solubility and CNS penetration

• Norepinephrine

• Epinephrine

In adrenergic system (sympathetic), what are the (2) neurotransmitters?

• Alpha (A1, A2)

• Beta (B1, B2, B3)

What are the (3) Receptors in Adrenergic System (Sympathetic)?

• Adrenergic Agonists

• Adrenergic Antagonists

What are the (2) drug categories of Adrenergic System (Sympathetic)?

• Epinephrine

• Phenylephrine

• Salbutamol

What are the (3) Examples of Adrenergic Agonists?

Hint: EPS

• Catechol ring

• Hydroxyl substitutions

• Amine side chain modifications

• Propranolol

• Prazosin

What are the (2) Examples of Adrenergic Antagonists?

Hint: EPS

• Aryloxypropanolamine structure

• Selectivity of beta blockers

• Serotonin

• Dopamine

• Noradrenaline

• GABA

• Acetylcholine

• Glutamic acid

What are the (6) Hormones and Mood Neurotransmitters?

Hint: Surigao del Norte GAG

Serotonin

What is the hormone for happiness, mood?

Dopamine

What is the hormone for motivation, pleasure?

Noradrenaline

What is the hormone for energy, concentration?

GABA

What is the hormone for calmness, anti-stress?

Acetylcholine

What is the hormone for memory, attention?

Glutamic acid

What is the hormone for learning, memory?

1. Neurotransmitter

2. Postsynaptic neuron

The presynapic neuron releases a (1)_____, which activates receptors on the (2)__________.

• Lipophilicity

• Molecular size

• Degree of ionization

• Hydrogen bonding

What are the (4) Important Factors Affecting Drug Penetration?

Hint: LIMO-DEHY

True

True or False: Polar drugs poorly cross the blood-brain-barrier (BBB).

• Sedatives and Hypnotics

• Antidepressants

• Antipsychotics

• Anticonvulsants

What are the (4) Major CNS Drug Classes?

Hint: SAAA

• Diazepam

• Phenobarbital

What are the (2) Examples of Sedatives and Hypnotics?

Hint: DIA-PHER

• Benzodiazepine ring system

• Barbituric acid derivatives

• Interaction with GABA receptors

• Fluoxetine

• Amitriptyline

What are the (2) Antidepressants?

Hint: FLU-AM

• Tricyclic structure

• Serotonin reuptake inhibition

• Lipophilic aromatic rings

• Chlorpromazine

• Haloperidol

What are the (2) Antipsychotics?

Hint: CHLO-HA

• Dopamine receptor antagonism

• Phenothiazine scaffold

• Phenytoin

• Valproic acid

What are the (2) Anticonvulsants?

Hint: PHEN-VAL

• Hydantoin ring

• Sodium channel inhibition

• Structure-activity relationships