Cholinergic

Receptor Subtype Nicotinic N Nicotinic M Location Response to Receptor Activation All autonomic nervous system ganglia Stimulation of parasympathetic and sympathetic postganglionic nerves and the adrenal medulla and release of epinephrine from the adrenal medulla Neuromuscular junction All parasympathetic target organs: Eye Heart Lung Contraction of skeletal muscle Contraction of the ciliary muscle focuses the lens for near vision Contraction of the iris sphincter muscle causes miosis (decreased pupil diameter) Decreased rate Constriction of bronchi Promotion of secretions Contraction of detrusor increases bladder pressure Relaxation of trigone and sphincter allows urine to leave the bladder Bladder Coordinated contraction of detrusor and relaxation of trigone and sphincter causes voiding of the bladder

Muscarinic

Salivation Increased gastric secretions Increased intestinal tone and motility Defecation Sweat glands* Generalized sweating Sex organs Erection Blood vessels Vasodilation * Although sweating is due primarily to stimulation of muscarinic receptors by acetylcholine, the nerves that supply acetylcholine to Cholinergic receptors on blood vessels are not associated with the nervous system. GI tract

Adrenergic
Receptor Subtype Eye Arterioles Skin Constriction Alpha1 Viscera Mucous membranes Veins Sex organs, male Prostate capsule Bladder Alpha2 Beta1 Presynaptic nerve terminals* Heart Kidney Arterioles Heart Dilation Lung Beta2 Skeletal muscle Bronchi Dilation Uterus Relaxation Liver Glycogenolysis Skeletal muscle Enhanced contraction, glycogenolysis Dopamine Kidney Dilation of kidney vasculature AV = atrioventricular, NE = norepinephrine, R = receptor. * Alpha2 receptors in the central nervous system are postsynaptic. Location Response to Receptor Activation Contraction of the radial muscle of the iris causes mydriasis (increased pupil size)

Constriction Ejaculation Contraction Contraction of trigone and sphincter Inhibition of transmitter release Increased rate Increased force of contraction Increased AV conduction velocity Renin release

Summary of Cholinergic Drugs and Their Receptors

Muscarinic Sweat glands Blood vessels Receptor Location All organs regulated by the parasympathetic nervous system Receptor Subtype NicotinicN All ganglia of the autonomic nervous system NicotinicM Neuromuscular junctions (NMJs)

Many, including: Effects of Receptor decreased Heart rate Promotes ganglionic Skeletal muscle Activation transmission contraction increased Gland secretion Smooth muscle contraction Bethanechol Nicotine (Nicotine*) Receptor Agonists Cholinesterase inhibitors: physostigmine, neostigmine (these drugs indirectly activate all cholinergic receptors) Receptor d -Tubocurarine, Atropine Mecamylamine Antagonists succinylcholine * The doses of nicotine needed to activate nicotinicM receptors of the NMJs are much higher than the doses needed to activate nicotinicN receptors in autonomic ganglia.

Mechanisms of Adrenergic Receptor Activation

Mechanism of Stimulation Direct Mechanism Binding to receptor to cause activation Indirect Mechanisms Promotion of NE release Inhibition of NE reuptake Inhibition of MAO Ephedrine* Amphetamines Cocaine Tricyclic antidepressants MAO inhibitors Examples Epinephrine Isoproterenol Ephedrine*

Categories of Cholinergic Drugs Category Representative Drugs Muscarinic agonists Bethanechol Muscarinic antagonists Atropine Ganglionic stimulating agents Nicotine Ganglionic blocking agents Mecamylamine Neuromuscular blocking agents Cholinesterase inhibitors d -Tubocurarine, succinylcholine Neostigmine, physostigmine