Exam 1

Sympathetic Innervation

ACH -> (N)

NE-> (α/β)

short-lomg

What are the parts of ACH?

  • 4° amine (ionic bonding)
  • Ethyline bridge (separation)
  • Ester (H-bond Acceptor, fragile)

 

Non-Depolarizing Ganglionic Antagonist (Nn)

  • bis 4º ammonium
  • 6 C separation
  • flexible

Neuromuscular blocker

 separation:

10 atoms separation between the 4º ammoniums

CNS blocker

separation:

6 atoms separation between the 4º ammoniums
Non-depolarizing competitive antagonist (Nm)

  • Bis-cation
  • ≥10 atoms separating the N(+)s
  • Separation rigid and bulky

Depolarizing competitive antagonist (Nm)

  • Bis 4? ammonium
  • 10 atoms separation
  • flexible

Where does ACH biosynthesis take place?
Presynaptically
Source of acetyl group
Acetyl COA
Enzyme that transfers acetyl group to choline in final stage

CHAT

(Choline Acetyltransferase)

Parasympathetic

ACH-> N

ACH-> M

Long-short

Nm receptor

α2 β1 γ δ

or

α2 β1 ε δ

Nn receptor
α2 β3
Broken down via Hoffman Degredation
Atracurium[image]9
Increased nicotinic receptor agonist activity
alkyl on α carbon
Increased muscarinic receptor agonist activity

alkyl substitution on β carbon

S config

Trans config

(also increased duration)

Ing’s rule

5 atoms: agonist

6-8 atoms: partial

9+ atoms: Antagonist

Muscarinic Antagonist

(Anticholinergics)

  1. Ring or bulk
  2. tertiary C with branched H bond (D/A)
  3. Spacer
  4. Cation

ACH binding to M1 M3 M5

Gq ; G11

Phospholipase C

IP3 DAG

;

ACH binding to M2 M4

G1

adenolate cyclase

decreased cAMP

;

G0

regulates K channels

L Tyrosine -; L-Dopa

Tyrosine Hydroxylase (Rate limiting)

Fe, O2, folate (cofactor)

L-Dopa -; Dopamine

LAAD (enzyme)

Pyridoxal Phosphate (Cofactor)

DA -; NE

Dopamine ; hydroxylase (Enzyme)

Cu O2 Vit C (Cofactor)

NE -; EP

Phenylethanolamine N-methyltransferase

SAM (Cofactor)

;1

Gq: activate PLC, hydrolysis of PIP2 to make DAG and IP3

Gca: regulate Ca channels

;2
Gi: inhibits adenolate cyclase ; decreases cAMP

1. MAO

2. Aldehyde reductase

NHR -; OH

1. MAO

2. Aldehyde dehydrogenase

CNHR -; COOH
COMT

(acts on one OH of catechol)

OH -; OCH3

1. Alcohol Dehydrogenase

2. Aldehyde dehydrogenase

COH -; COOH
x

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