Neuropharmacology Cheat Sheet

The core ideas of Neuropharmacology distilled into a single, scannable reference — perfect for review or quick lookup.

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Quick Reference

Neurotransmission

The process by which signaling molecules called neurotransmitters are released from the presynaptic neuron, cross the synaptic cleft, and bind to receptors on the postsynaptic neuron, thereby transmitting a chemical signal between nerve cells.

Receptor Agonism and Antagonism

An agonist is a drug that binds to a receptor and activates it to produce a biological response, while an antagonist binds to a receptor without activating it, blocking the action of endogenous ligands or other agonists.

Dose-Response Relationship

The quantitative relationship between the dose of a drug administered and the magnitude of the resulting pharmacological effect. It is typically represented as a sigmoidal curve plotting effect against log-dose.

Blood-Brain Barrier (BBB)

A highly selective semipermeable border of endothelial cells connected by tight junctions that separates circulating blood from the brain extracellular fluid, restricting the passage of most drugs and solutes into the central nervous system.

Synaptic Plasticity

The ability of synapses to strengthen or weaken over time in response to changes in activity levels. This is the neurobiological basis for learning and memory and a key target for cognitive-enhancing drugs.

Reuptake Inhibition

A pharmacological mechanism in which a drug blocks the reabsorption of a neurotransmitter back into the presynaptic neuron after it has been released into the synaptic cleft, thereby increasing the neurotransmitter's concentration and duration of action at the synapse.

Pharmacokinetics vs. Pharmacodynamics

Pharmacokinetics describes what the body does to a drug (absorption, distribution, metabolism, and excretion), while pharmacodynamics describes what the drug does to the body (mechanism of action, receptor interactions, and downstream effects).

Tolerance and Dependence

Tolerance is the diminished response to a drug after repeated exposure, requiring increased doses to achieve the same effect. Physical dependence occurs when the body adapts to the drug's presence and withdrawal symptoms emerge upon discontinuation.

Allosteric Modulation

The regulation of a receptor's activity by the binding of a modulator at a site distinct from the orthosteric (primary) binding site. Positive allosteric modulators enhance the receptor's response to its natural ligand, while negative allosteric modulators reduce it.

Neurotransmitter Systems

Organized networks of neurons that synthesize, release, and respond to specific neurotransmitters. Major systems include the dopaminergic, serotonergic, noradrenergic, cholinergic, GABAergic, and glutamatergic systems, each regulating distinct physiological and behavioral functions.

Key Terms at a Glance

Acetylcholine:A neurotransmitter that activates nicotinic and muscarinic receptors, mediating neuromuscular transmission, autonomic function, and central processes like memory and attention.

Agonist:A chemical that binds to a receptor and activates it to produce a biological response, mimicking the action of the endogenous ligand.

Allosteric Modulation:The regulation of a protein's activity by binding of an effector molecule at a site other than the protein's active (orthosteric) site.

Antagonist:A substance that binds to a receptor without activating it, blocking the action of agonists and endogenous ligands.

Blood-Brain Barrier:A highly selective semipermeable barrier formed by tight junctions of brain capillary endothelial cells that prevents most circulating substances from entering the brain.

Catecholamine:A class of monoamine neurotransmitters derived from the amino acid tyrosine, including dopamine, norepinephrine, and epinephrine.

Cyclic AMP (cAMP):A second messenger molecule generated from ATP by the enzyme adenylyl cyclase upon GPCR activation. It activates protein kinase A (PKA) to phosphorylate target proteins.

Dopamine:A catecholamine neurotransmitter critically involved in reward, motivation, motor control, and cognition. Dysregulation is implicated in Parkinson's disease, schizophrenia, and addiction.

Dose-Response Curve:A graphical representation of the relationship between drug dose (or concentration) and the magnitude of the pharmacological effect, typically sigmoidal in shape.

EC50:The effective concentration of a drug that produces 50% of the maximum possible response. A measure of drug potency.

Excitotoxicity:Neuronal injury and death resulting from excessive activation of excitatory amino acid receptors, primarily by glutamate, leading to toxic intracellular calcium levels.

GABA:Gamma-aminobutyric acid, the principal inhibitory neurotransmitter in the adult mammalian central nervous system. Synthesized from glutamate by the enzyme glutamic acid decarboxylase.

Glutamate:The most abundant excitatory neurotransmitter in the central nervous system, acting on ionotropic (AMPA, NMDA, kainate) and metabotropic receptors.

G-Protein-Coupled Receptor:A large superfamily of transmembrane receptors that detect extracellular molecules and activate intracellular signal transduction pathways through heterotrimeric G-proteins.

Half-Life:The time required for the plasma concentration of a drug to decrease by 50%. It determines dosing frequency and the time to reach steady-state concentrations.

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