Described the actions of the esters and ethers of choline on isolated organs and their relationship to muscarinic, pharmacologist, physiologists, chemists, and
biochemists have applied their knowledge to understand the actions of the cholinergic nerve and its neurotransmitter
Dale
Found in the Central and Peripheral nervous system and use Ach as their neurotransmitter
Cholinergic Receptor
Cholinergic receptors use ____ as neurotransmitter
Ach
2 kinds of cholinergic receptor
Nicotinic
Muscarinic
Ionotropic receptors or Ligand-gated ion channels
Responsive to Ach and Nicotine
Nicotinic
Metabolic receptors or G-protein couple receptors
Responsive to Ach and Muscarine
Muscarinic
2 subtype of Ncotinic Cholinergic Receptors
Ganglionic receptor (neural) N2
Muscle receptor (somatic) N1
Ganglionic receptor (neural) N2 is blocked by ______ and ________ but stimulated by __________ and ___________
hexamethonium
trimethaphan
tetramethylammonium
dimethyl 4-phenylpiperazinium
Muscle receptor (somatic) N1 is blocked by ______, _______ and ________ and stimulated by ________
succinycholine
d-tubocurarine
decamethonium
phenyltrimethylammonium
Muscle receptor (somatic) N1 is blocked by ______, _______ and ________ and stimulated by ________
succinycholine
d-tubocurarine
decamethonium
phenyltrimethylammonium
Post synaptic on neuromuscular junctions
Muscle receptor (somatic) N1
Found in both the CNS and PNS
Ganglionic receptor (neural) N2
responsible for transmission at sympathetic and
parasympathetic ganglia
Ganglionic receptor (neural) N2
responsible for skeletal muscle contraction
Muscle receptor (somatic) N1
Second-messenge systems that cause muscle contraction
Phosphoinositol system
Second-messenge systems that cause smooth muscle relaxation
Adenylate cyclase
Second-messenge systems that slows heart rate
Ion channels
provide the primary source of acetylcholine to
the cerebral cortex, and are known for their role in promoting cortical activation during both wakefulness and during rapid eye movement (REM) sleep
Cholinergic Neurons
the specific study of neurochemicals including neurotransmitters and other molecules (such as psychopharmaceuticals) that influence the function of neurons
Neurochemistry
is the study of the chemistry involved
in the relative spatial arrangement of atoms and molecules
Stereochemistry
study of spatial arrange of cholinergic atoms and molecules
Cholinergic Stereochemistry
is a method of determining the arrangement of atoms within a crystal, in which a beam of X-rays strikes a crystal and diffracts into many specific directions
X-ray crystallography
a physical phenomenon in which nuclei in a magnetic field absorb and re-emit electromagnetic radiation
Nuclear magnetic resonance
encompasses all theoretical methods and computational techniques used to model or
mimic the behaviour of molecules.
Molecular modeling by computation
The study of the relationship between
a drug's molecular structure and the drug's biological activity
Structure Activity Relationship
Receptors that block synapses of the parasympathetic nerves
Cholinergic Receptor Antagonists
other name of cholinergic antagonist
cholinergic blockers, parasympatholytics or
anticholinergic
inhibit the cholinesterase enzyme from breaking
down ACh, increasing both the level and duration of the neurotransmitter action
AChE inhibitors or anti-cholinesterases
is an enzyme that specifically cleaves Ach to acetate and choline and, thus, terminates its actions
Acetylcholinesterase
2 types of cholinesterases in humans
Butyrylcholinesterase
(BuChE)
Acetylcholinesterase
(AChE)
2 groups of AChEi
Reversible Inhibitors
Irreversible Inhibitors
Agents that block the transmission of ACh at the
motor end plate
NEUROMUSCULAR BLOCKING AGENTS
depolarize the membrane of the muscle end plate.
Depolarizing Blocking Agents
was a term used to describe collectively the
very potent arrow poisons used since early times by the South American Indians
curare