Autonomic Receptors
Structural family Functional families Receptor Physiological ligands Effectors, Transducers, Major functions G Protein Coupled Receptors (GPCR) Muscarinic receptors M1 Acetylcholine Gq-coupled Increased phospholipase C increased IP3, diacylglycerol, cytoplasmic calcium M2 Acetylcholine Gi-coupled Decreased adenylyl cyclase decreased cAMP M3 Acetylcholine Gq-coupled Increased phospholipase C increased IP3, diacylglycerol, cytoplasmic calcium Alpha-adrenergic receptors Alpha1 (α1) Epinephrine, norepinephrine Gq-coupled Increased […]
The Effects of the Autonomic Nervous System on Organ Systems
Sympathetic Parasympathetic Organ Target Actiona Receptorb Actiona Receptorb Eye Iris Radial muscle Contracts α1 — — Circular muscle — — Contracts M3 Ciliary muscle [Relaxes] β Contracts M3 Heart Sinoatrial node Accelerates β1, β2 Decelerates M2 Ectopic pacemakers Accelerates β1, β2 — — Contractility Increases β1, β2 Decreases (atria) [M2] Blood vessels Skin, splanchnic vessels […]
Cellular Receptors of Relevance to Therapeutics
This table provides a summary of the various types of cellular receptors that are drug targets. Classes Subclasses or families Physiological ligands Transducers, principal effects, or ions G protein-coupled receptors (GPCRs)a Adhesion Frizzled Glutamate Rhodopsin Secretin Very large number of endocrine and paracrine factors, but other types of ligands as well G proteins Gs: Adenylyl […]
Pharmacology
Pharmacology Resources
Common drug stems This table provides common drug stems to quickly help you determine to which class a medication belongs. GO TO Monoclonal Antibody Naming Convention slides Handouts The following pharmacology handouts are graciously being shared with WSU College of Medicine students by Dr. John Szarek. If you would like to utilize these handouts, you […]
References
Books + Journals Chapter 6 Introduction to Autonomic Pharmacology, Katzung BG, Kruidering-Hall M, Tuan R, Vanderah TW, Trevor AJ. Katzung & Trevor’s Pharmacology: Examination & Board Review, 13e; 2021. Accessed: September 13, 2022. Leurs, R. et al. The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nature Reviews Drug Discovery 4, 107-120 (2005). All […]
Self-Assessment
Quiz Question A drug is an alpha-1 adrenergic receptor agonist. Which effect would you expect the drug to have on vascular smooth muscle? Question A drug is an alpha-1 adrenergic receptor antagonist. Which effect would you expect the drug to have on vascular smooth muscle? Question A drug is a beta-1 receptor agonist. Which effect […]
Predict Therapeutic and Adverse Effects
The following table summarizes receptor types along with potential agonists and antagonists. Please note the agonists and antagonists listed are not all encompassing. Receptor Type Agonists Antagonists GProtein Linked Enzyme Second Messenger N1 nicotinic ACh ACh (nicotine, decamethonium) d-Tubocurarine, α-bungarotoxin N2 nicotinic ACh ACh (nicotine, TMA) Hexamethonium M1/M3/M5 muscarinic ACh ACh (muscarine) Atropine, pirenzepine (M1) Gαq PLC […]
Activation of the Autonomic Neurons
Activation of autonomic neurons leads to different effects depending on the target organ system. A table consolidating the effect each division of the autonomic nervous system has on specific organ systems is provided below. Eye Heart Blood vessels Bronchiolar Gastrointestinal Genitourinary smooth muscle Skin Sweat glands Metabolic Function Autonomic Nerve Endings aLess important actions are […]
Major Receptors in the ANS
The major receptors in the Autonomic Nervous System include cholinergic and adrenergic receptors. Cholinergic Receptors (Cholinoreceptors) Cholinergic receptors respond to ACh, and its analogs, and are classified as muscarinic (respond to muscarine and ACh) or nicotinic (respond to muscarine and ACh). M1 Receptor Location Mechanism Major Function Nerve endings Gq-Coupled Increased phospholipase C→increased IP3, diacylglycerol, […]