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Nicotinic receptors
NM NN Central N
Location Skeletal NMJ post synaptic
All autonamic ganglia and adrenal medulla
Sensory nerve terminals presynaptically
Function Contraction of Sk. muscle
NE & E from adrenal medulla
Facilitate release of Dopamine, glutamate
Mechanism Ligand gated channel
Ligand gated channel
Acetyl Co enzyme A and Choline.
M1 (Neuronal and gastric)
M2 (Cardiac) M3(Glandular) M4 M5
Distribution
Ganglia, gastric parietal cells, CNS (cortex, hippocampus)
Myocardium, smooth muscle, presynaptic PNS,CNS
Exocrine glands, visceral smooth muscle, vascular endothelium
Neostriatum Substantia nigra
Function
Gastric acid secretion, GI motility, CNS excitation
SA node rate of impulse generationAV node velocity and decrease atrial and ventricular contraction
Exocrine secretions. Smooth muscle contraction (expect urinary, Blood vessels
- -
Mech G protein (Gq), IP3,DAG,depolarization
Gi cAmp, opening of K+ channels
G protein (Gq), IP3,DAG,depolarization
Gi cAmp, opening of K+ channels
G (Gq), IP3,DAG,depolariz
Agonist
Oxotremorine Methacholine Bethanechol - -
Anta gonist
Pirenzepine, Telenzepine
Methoctramine,Tripitramine
4-DAMP, Hexa hydrosiladifenidol
CENTRAL NERVOUS SYSTEMBrain
PARASYMPATHETIC
Spinalcord
Stimulates salivation VII
Constricts bronchi X
Slows heartbeat X
Stimulates activity
Contracts bladder
Stimulates erectionof sex organs S
Stimulates gallbladder
Gallbladder
Contracts pupil III
Parasympathomimetics
Directly acting Indirectly acting 1. Ach2. Synthetic choline esters Reversible Irreversible
Methacholine CarbamatesCarbachol 1. Natural alkaloids 1. OrganophosphatesBethanechol
3. Natural alkaloids 2. Quaternary
4.Miscellaneous 2. Carbamates
Acridine Tacrine
• Edrophonium• Neostigmine• Pyridostigmine• Ambenonium• Demecarium• Rivastigmine • Popoxour
• Carbaryl• Tremorine• Oxotremorine
• Muscarine• Nicotine• Pilocarpine• Arecoline
• Physostigmine • Ecothophate• Isoflurophate• Paraoxon• Parathion• Malathion• Diazon
Anger, Alert,
Aggressive
Flushing of Face
Bronchodilatation
Mydriasis
In. Cardiac output
Inc. Muscle tone
Lipolysis-Energy
Liver GlucogenolysisMore energy prod
Large B vessels dilate to speed up blood flow
Tyrosine→Dopa→Dopamine→NEpi→Epi