Phramacology Cholinergic Transmission

Front 1

acethlcholine synthesis happens where?

Back 1

in the cholinergic nerve terminal cytoplasm

Front 2

Ach synthesized by the action of?

Back 2

enzyme Choline Acetyltransferase (ChAT) on the precursors choline (Ch) and acetylcoenzyme A (acetyl-CoA)

Front 3

choline is provided mainly through?

Back 3

high-affinity sodium co-transport pumps (which require energy) located on the nerve terminal membrane

Front 4

De Novo synthesis of Ch

Back 4

occur to a limited extent
from choline-containing phospholipids
acts to provide enough Ch to make up for amt. lost in the synapse

Front 5

Acetyl-CoA is synthesized from?

Back 5

pyruvate & acetate, acetylating coenzyme A in mitochondoria

Front 6

Hemicholinium-3 (HC-3) inhibits?

Back 6

inhibit high affinity uptake carriers of Ch
leads to eventual depletion of Ach in the nerve terminal

Front 7

Vesamicol inhibits?

Back 7

inhibits Ach transport system on the vesicles

Front 8

Botulinium Toxin (Bo Tox)

Back 8

binds to sites on the nerve terminal
causes irreversible inhibition of the release of Ach from the nerve terminal

Front 9

Bo Tox blocks?

Back 9

blocks the ability of Ach vesicles to fuse with the internal nerve terminal cell wall and excytosis

Front 10

black widow spider venom

Back 10

triggers the exocytosis of Ach-containing vesicles

Front 11

acetylcholinesterase catabolizes Ach to?

Back 11

Ch and acetic acid

Front 12

2 cholinergic receptors

Back 12

muscarinic and nicotinic

Front 13

muscarinic receptors

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comprised of a family of receptors (M1-M5)

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M1 location?

Back 14

in autonomic ganglia and CNS

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M2 location?

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on supraventricular regions of heart

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M3 location?

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on smooth muscles
glands
vascular endothelial cells

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M1 & M3 are coupled to?

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phospholipase C via G proteins

Front 18

phosphatidylinositol polyphosphates(PIP)spilits into?

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inositol 1,4,5 triphosphate (IP3) &
Diacylglycerol (DAG)
by activation of M1 & M3 receptors

Front 19

IP3

Back 19

water soluble (in cytoplasm)
act on IP3 receptors on the sarcoplasmic reticulum &
increase Ca release

Front 20

DAG

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lipid soluble (in cell memb)
along with increase Ca,
activates protein kinase C (PKC)

Front 21

muscarinic Ach receptors

Back 21

belong to a class of metabotropic receptors which use G proteins as their signalling mechanism

Front 22

nicotinic receptors

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use an ion-gated mechanism for signalling

Front 23

Muscarinic receptors are found in?

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parasympathetic nervous system

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M1

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late EPSP in ganglia
blocked by Atoropine
selectively stimulated by Oxotremorine

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EPSP

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excitatory post-synaptic potential

Front 26

Pirenzepine

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fairly selective M1 antagonist

Front 27

M2

Back 27

mainly cardiac (decreases AV nodal conduction & SA automaticity, < HR)
blocked by Atropine

Front 28

AF-DX116

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selective M2 antagonist

Front 29

M3

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mainly at neuroeffector junctions (glands, smooth muscles)
blocked by Atropine

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M3

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exsalivation
urination
defecation
pupillary constriction
bronchoconstriction

Front 31

Hexahydrosilafenidol

Back 31

selective M3 antagonist

Front 32

M4

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mainly in CNS
antagonized by Himbacine

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M5

Back 33

exact importance and locations still unclear

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nicotinic receptors

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ganglionic receptors in both symp/para-symp and neuromuscular junctions

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ganglionic nicotinic receptors stimulated by?

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Ach & Dimethylphenyl-piperazinium (DMPP)

Front 36

ganglionic nicotinic receptors antagonized by?

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Trimethaphan (Arfonad)

Front 37

neuromuscular nicotinic receptors stimulated by?

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nicotine and Ach

Front 38

Phenyltrimetyl ammonium (PTMA)

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a selective agonist of neuromuscular nicotinic receptor

Front 39

D-tubocurarine (Tubarine)

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a non-depolarizing antagonist of neuromuscular nicotinic receptor

Front 40

alpha-bungarotoxin

Back 40

from snake venom
almost irreversible antagonist of neuromuscular nicotinic receptor

Front 41

neuromuscular depolarizing blockers

Back 41

Decamethonium
Succ (Anectine)
initially stimulate receptor, then block

Front 42

autoreceptors

Back 42

mainly muscarinic (M1, M2, ??)
inhibit further release of Ach
nicotinic autoreceptors found, but they tend to increase rather than inhibit Ach release

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heteroreceptors

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innervention on nerve terminal by another type of receptor
allows control of release by another system
receptors react to circulating neurotransmitter

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cycloplegia

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paralysis of accomodation from para-symp drug

Front 45

contraction of ciliary muscle

Back 45

release the tension of suspensaory ligament
lens get thicker

Front 46

relaxation of ciliary muscle

Back 46

pulls ligament
makes lens thinner