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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
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Found in the Central and Peripheral nervous system and use Ach as their neurotransmitter
Cholinergic Receptor
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Cholinergic receptors use ____ as neurotransmitter
Ach
-
2 kinds of cholinergic receptor
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Ionotropic receptors or Ligand-gated ion channels
Responsive to Ach and Nicotine
Nicotinic
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Metabolic receptors or G-protein couple receptors
Responsive to Ach and Muscarine
Muscarinic
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2 subtype of Ncotinic Cholinergic Receptors
Ganglionic receptor (neural) N2
Muscle receptor (somatic) N1
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Ganglionic receptor (neural) N2 is blocked by ______ and ________ but stimulated by __________ and ___________
hexamethonium
trimethaphan
tetramethylammonium
dimethyl 4-phenylpiperazinium
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Muscle receptor (somatic) N1 is blocked by ______, _______ and ________ and stimulated by ________
- succinycholine
- d-tubocurarine
- decamethonium
phenyltrimethylammonium
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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
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Found in both the CNS and PNS
Ganglionic receptor (neural) N2
-
responsible for transmission at sympathetic and
parasympathetic ganglia
Ganglionic receptor (neural) N2
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responsible for skeletal muscle contraction
Muscle receptor (somatic) N1
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Second-messenge systems that cause muscle contraction
Phosphoinositol system
-
Second-messenge systems that cause smooth muscle relaxation
Adenylate cyclase
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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
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the specific study of neurochemicals including neurotransmitters and other molecules (such as psychopharmaceuticals) that influence the function of neurons
Neurochemistry
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is the study of the chemistry involved
in the relative spatial arrangement of atoms and molecules
Stereochemistry
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study of spatial arrange of cholinergic atoms and molecules
Cholinergic Stereochemistry
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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
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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
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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)
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2 groups of AChEi
Reversible Inhibitors
Irreversible Inhibitors
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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
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was a term used to describe collectively the
very potent arrow poisons used since early times by the South American Indians
curare
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