Skip to content
Pharm Academy
English

Receptor theory and drug targets

Classification of pharmacodynamic targets

Pharmacodynamics examines how medicines produce their effects in the body and the molecular or physicochemical mechanisms through which they modify biological functions.

Drug targets are most commonly proteins. However, nucleic acids, components of pathogens, and non-specific chemical or physical interactions may also contribute to a drug’s effects.

Important: the following examples help organise the major types of drug targets. A medicine may have several targets and more than one mechanism of action.
Main category Target group Target type Specific target or mechanism Example medicine
Proteins Ion channel Voltage-gated ion channel Voltage-gated Na⁺ channel Lidocaine
L-type Ca²⁺ channel Amlodipine
Enzyme Catalytic protein Angiotensin-converting enzyme (ACE) Ramipril
Cyclooxygenase enzymes (COX) Ibuprofen
Transport protein and pump Membrane transporter Serotonin transporter (SERT) Fluoxetine
Sodium-glucose cotransporter 2 (SGLT2) Remogliflozin
Ion pump Gastric H⁺/K⁺-ATPase proton pump Pantoprazole
Receptor Ion channel receptor GABAA receptor, ligand-gated Cl⁻ channel Diazepam
NMDA receptor, ligand-gated cation channel Memantine
Intracellular ryanodine receptor, the Ca²⁺-release channel of the endoplasmic reticulum Dantrolene
Enzyme-linked receptor Receptor tyrosine kinase: epidermal growth factor receptor (EGFR) Erlotinib
Receptor tyrosine kinase: anaplastic lymphoma kinase (ALK) Crizotinib
Receptor serine/threonine kinase: transforming growth factor-β receptor type I (TGFBR1/ALK5) Galunisertib*
Receptor-associated cytoplasmic tyrosine kinase: cytokine receptor–JAK1/JAK2 signalling Ruxolitinib
Membrane-bound receptor guanylate cyclase: natriuretic peptide receptor A (NPR-A) Nesiritide
G protein-coupled receptor Gs-coupled β2-adrenoceptor Salbutamol
Gq-coupled M3 muscarinic receptor Oxybutynin
Gi-coupled α2-adrenoceptor Clonidine
Nuclear receptor Oestrogen receptor Tamoxifen
Structural protein Cytoskeletal component Microtubules Vincristine
Other macromolecule Nucleic acid DNA Formation of DNA cross-links Cisplatin
Physicochemical and non-specific action Acid–base reaction Antacid Chemical neutralisation of gastric acid Magnesium hydroxide
Binding in the intestine Bile acid sequestrant Binding of bile acids in the intestine Colestyramine
Biological neutralisation Antitoxin Neutralisation of a bacterial toxin Tetanus antitoxin
Complex formation Chelating agent Binding of heavy-metal ions Dimercaprol
Physical contrast effect Diagnostic contrast medium Absorption of X-rays Barium sulfate
Pathogen-related targets Bacterium Enzyme DNA gyrase and topoisomerase IV Ciprofloxacin
Virus Enzyme HIV reverse transcriptase Efavirenz
Fungus Biosynthetic enzyme system Ergosterol biosynthesis Fluconazole
Protozoan Enzyme Plasmodium falciparum dihydrofolate reductase Pyrimethamine
Helminth Ion channel Glutamate-gated Cl⁻ channel Ivermectin

* Galunisertib is an investigational medicine and is included as an example of the pharmacological modulation of a receptor serine/threonine kinase.

Sacubitril does not act directly on a receptor guanylate cyclase. By inhibiting neprilysin, it increases the concentrations of several natriuretic peptides, which can subsequently activate the corresponding receptor guanylate cyclases.

You need to be logged in to view this exercise.