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FUNCTION:
contraction of skeletal muscles
NM RECEPTORS
MECHANISM:
Ligand gated ion channel- opening of cation
(Na+) channel (end plate depolarization.
NN RECEPTORS
LOCATION:
At all autonomic ganglia and at adrenal
medulla, post synaptic
FUNCTION:
Transmission of impulse through the
autonomic ganglia and firing of post ganglionic
neuron
Secretion of norepinephrine and
epinepherine from adrenal medulla.
NN RECEPTORS
MECHANISM:
Ligand gated ion channel- opening of cation
(Na+) channel (end plate depolarization)
MUSCARINIC RECEPTORS
•Cholinergic transmission (acetylcholine-
mediated) that activates muscarinic receptors
occurs mainly at autonomic ganglia, organs
innervated by the parasympathetic division of the
autonomic nervous system and in the central
nervous system.
MUSCARINIC RECEPTORS
•All muscarinic receptors are G-protein coupled
receptors.
•Studies have identified five subclasses of
muscarinic receptors: M1,M2, M3, M4, and M5.
CLASSIFICATION
LOCATION AND FUNCTION
•M1, M4 and M5 receptors: CNS. These receptors are
involved in complex CNS responses such as memory,
arousal, attention and analgesia. M1 receptors are also
found at gastric parietal cells and autonomic ganglia.
•Alpha Receptors
1. Alpha-1
2. Alpha-2
•Beta Receptors
1. Beta-1
2. Beta-2
3. Beta-3
LOCATION:
Vascular smooth muscles, gut, genitourinary
smooth muscle , liver.
LOCATION:
pancreatic b-cells, platelets, nerve
terminals
LOCATION:
Heart.
BETA-2 RECEPTORS:
LOCATION:
Vascular smooth muscles, bronchial, gut
and genito urinary.
RESPONSE:
Relaxation.
BETA-3 RECEPTORS
LOCATION:
Adipose Tissue.
RESPONSE:
Lipolysis
• All muscarinic receptors appear to be G- protein
coupled receptors.
•In case of M1,M3 and M5 receptors the binding of
the muscarinic receptors activate the
inositolphosphate(IP3), diacyl glycerol (DAG)
cascade.
•DAG helps in the opening of the smooth muscle
calcium channels; IP3 releases calcium from
endoplasmic reticulum and sarcoplasmic reticulum.
• Muscarinic activation in some tissues like
heart, intestine inhibits the adenyl cyclase activity.
•These include the receptors present on M2 and M4.
• These produces the activation and opening of
potassium channels.
•Thereby it inhibits the neuronal calcium levels.
•These muscarinic effects on cAMP generation reduce
the physiological response of the organ to stimulatory
hormone.
• The neuronal nicotinic receptor consists of alpha
and beta subunits only.
• Each subunit has four transmembrane segments.
• Agonist binding to the receptor sites causes a
conformational change in the protein( channel
opening) that allows Na+ and K+ ions to diffuse
rapidly down their concentration gradients ( calcium
ions may also carry charge through the nicotine
receptor ion channel).
•Binding of an agonist molecule by one of the two
receptors sites increases the probability of channel
opening ;simultaneously binding of the agonist by
both of the receptors sites enhances opening
probability.
• Nicotinic receptor activation causes
depolarization of the nerve cell or neuro muscular
end plate membrane .
• In skeletal muscle; the depolarization propagates
across the muscle membrane and causes
contraction.
• Alpha-1 receptors are coupled via G proteins in
the family to phospholipase C.
• This enzyme hydrolyses polyphosphoinositides
leading to the formation of inositol 1,4,5
triphosphate (IP3) and diacylglycerol(DAG).
• IP3 promotes the release of Ca2+ from the
intracellular stores which increases the cytoplasmic
concentration of free Ca2+ and activation of
various calcium dependent protein kinases.
• Activation of these receptors may increase the
influx of Ca2+ across the cells plasma
membrane.
•IP3 is sequentially dephosphorylated leads to
the formation of free inositol.
• DAG activates protein kinase C, which
modulates the activity of signalling pathway.
• Alpha-2 receptors inhibit adenyl cyclase activity
and intracellular cyclic adenosine monophosphate
(cAMP) levels to decrease.
• Alpha-2 receptor mediated inhibition of adenyl
cyclase activity is transduced by the inhibitory
regulatory protein, G1.
• Alpha-2 receptor agonists cause platelet
aggregation and decrease in platelet cAMP levels.
• They use other signaling pathways including
regulation of ion channel activities and activities of
important enzymes involved in signal transduction.
• Activation of all three receptor ( beta-1,beta-2 and
beta-3) results in stimulation of adenyl cyclase and
increased conversion of ATP to cAMP.
•cAMP is the major secondary messenger of beta-
receptor activation.
•Eg: liver, beta receptors activation of glycogen
phsphorylase.
• heart, beta receptors promotes the relaxation
of smooth muscles.
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