This is from GurunanakCollege of Pharmacy, Nagpur.
This Presentation is created by Sheikh Amaan.
This is under the Partisipative learning.
B.Pharm 4th Semester
2. INTRODUCTION
• Neurotranmitters:
A chemical substance which is released at the end of a nerve fiber by the arrival of a
nerve impulse and, by diffusing across the synapse or junction, effects the transfer of
the impulse to another nerve fiber, a muscle fiber, or some other structure.
• The cholinergic system: It composed of organized nerve cells that use the
neurotransmitter acetylcholine in the transduction of action potentials. These
nerve cells are activated by or contain and release acetylcholine during the
propagation of a nerve impulse.
• Acetylcholine is major neurotransmitter of parasympathetic division of
autonomic nervous system.
4. BIOSYNTHESIS AND CATABOLISM OF ACETYLCHOLINE
• The chemical transmitter at both pre and postganglionic synapses in the parasympathetic
system is acetylcholine (ach).
• Ach is also the neurotransmitter at sympathetic preganglionic synapses, some sympathe
neuromuscular junction (somatic nervous system), and at some sites in the CNS.
• Acetylcholine is the most widespread autonomic transmitter present in the body.
• Ach is released into the synaptic vesicle of effectors junction by an impulse across the
neuroeffector junction this leads to action potential due to the difference in the ionic
gradients of Na+ and K+ and in other tissues it is mediated along with calcium ion.
• Ach is synthesis locally in cholinergic nerve ending by adenosine-tri phosphate(ATP)
dependent system.
5. BIOSYNTHESIS OF ACETYLCHOLINE
• It was first synthesized by Bayer in 1867.
• Synthesis of Ach involves reaction of choline with active acetyl Co-A.
• Active acetyl Co-A being formed by the combination of acetate with coenzyme-A.
S-Adenosyl methionine act as methyl donor
Acetyl CoA act as acetyl donor.
6. • The reaction between acetyl coenzyme A and choline is catalyzed by the enzyme
cholineacetylase.
• There is considerable evidence that the enzyme cholinacetylase is synthesized
within the neuronal perikaryon, then transferred along the axon to its terminals
where the formation of acetylcholine is believed to occur.
9. CHOLINESTERASE
• Immediately after release of ach, ach is hydrolyzed by enzyme cholinesterase
and choline is recycled.
• A specific acetylcholine-esterase or true cholinesterase brings about process of
termination of Ach function i.e. stop its activity.
• A non specific butyrylcholinesterase-BuChE or pseudo cholinesterase brings
about hydrolysis of ingested (out side) esters.
10. CHOLINERGIC RECEPTORS AND THEIR
DISTRIBUTION
• CHOLINERGIC RECEPTORS ARE MUSCARINIC AND NICOTINIC RECEPTORS
• MUSCARINIC RECEPTOR:
THESE ARE STIMULATED BY MUSCARINE AND BLOCKED BY ATROPINE.
MUSCARINE RECEPTOR ARE OF 5 TYPES.
M1
M2
M3
M4
M5
11.
12. NICOTINIC RECEPTOR
• These receptor are selectively activated by nicotine and blocked by tubocurarine or
hexamethonium.
• They are rosette-like pentameric structure which enclose ligand gated cation channel.
• They are of two subtypes:
• Nm
• DISTRIBUTION=They are present at skeletal muscle end plate.
• Are stimulated by phenyltrimethanammonium(PTMA)
• Blocked by tubocurarine
• Mediate skeletal muscle contraction.
• Nn
• DISTRIBUTION=Are present on ganglionic cells (sympathetic & parasympathetic), adrenal medullary cells
and spinal cord and in certain areas of brain.
• Are stimulated by di-methyl phenyl piperazinium (DMPP)
• Blocked by hexamethonium
• Constitute the primary pathway of transmission in ganglia