Med chem exam 2

Duration of ?1 antagonists

 

Ester: shortest acting

Amide: Intermediate acting

Ether: longest acting

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Aryloxypropanolamine

Tricyclic antidepressents

2° amine:

3° amine:

2° amine: NE uptake blocker

3° amine: 5HT uptake blocker

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Cocaine

blocks reuptake of NE & DA

Enzyme that turns L-DOPA into Dopamine
LAAAD
Rate limiting enzyme for DA synthesis
Tyrosine Hydroxylase
D1/D5 receptor

  • Activates adenylate cyclase
  • ^cAMP

D2, D3, D4

  • Pre & post synaptic
  • Inhibit adenylate cyclase
  • vcAMP

? Rotamer

  • Same side
  • D1 = D2

? Rotamer

  • Opposite side
  • D2 > D1

COMT

(+SAM)

OH -> OCH3

MAO
amine -> Aldehyde
Aldehyde dehydrogenase

(+NAD)

Aldehyde -> Carboxylic acid

How do D2 autoreceptors inhibit DA?

 

  • Inhibit synthesis (Tyrosine hydroxylase)
  • Inhibit release

Basal Ganglia

  • Substantia Nigra origin of corpus striatum)
  • controls posture, muscle tone, movement
  • Lack = Parkinson’s, EPS.
  • (ACH works with DA for balance)

Meso-Limbic system

  • Behavior & Emotion
  • Too much: Schizophrenia (Psychosis)
  • Too few: Depression

Tubero-infundibular system

  • Anterior pituitary
  • DA decreases prolactin release

Meso-accumbens pathway

  • DA controls locomotion

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  • ^ DA release
  • v DA uptake

Taken up actively by presynaptic neurons

(Parkinsin’s)

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  • Mimics GABA
  • CNS suppression (v DA)

DA agonist uses

  • Primary: Parkinson’s
  • secondary: RLS (Requip/Mirapex)

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DA agonist

NOTE:

  1. Aromatic ring
  2. Basic N (separated from AR by 2 atoms)
  3. Minimal bulk
  4. ? rotomeric

DA antagonist uses

  • Primary: Antipsychotics
  • Minor: Anti-emetic (Metoclopramide)
  • Adjuvent: Depression/Bipolar

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Phenothiazine

NOTE

  • S
  • separation of 2-4 between AR and N
  • Cl = EWG = required.

Phenothiazine

Preferd activity

3; amine ; 4; amine ; Sulfonium ; Thioether
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Tyrosine Hydroxylase inhibitor

NOTE:

  • Extra methyl group prevents enzyme from acting (reversible inhibition)

Treat pheochromocytoma (excess NE/E)

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LAAAAD inhibitor

NOTE:

  • Extra methyl group.; converted by LAAAAD into a false NT
  • Presynaptic ;2 agonist (; BP)

;

; mediates

smooth muscle contraction

  • Agonist:decongestion, vasoconstriction
  • A1 Antagonist: treat hypertension ; BPH
  • A2 Antagonist: treat depression

;

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Phenethanolamine

NOTE:

OH

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2-arylImidazoline

NOTE:

C

;1 agonist

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Phenethylamine (Amphetamine)

NOTE:

no OH

Indirect acting ;1 agonist (promote NE release)

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2-aminoimidazoline (Clonidine)

NOTE:

ortho N, Halogen,

;2 agonist

CNS antihypertensives.;

;

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Imidazole based ;2 agonist

NOTE:

benzene substituants are O ; M

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Imidazoline

NOTE:

No halogen

; antagonist

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;-Haloalkylamine

;2 antagonist irreversible

NOTE:

ether

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Quinazoline (Doxazosin, longest acting)

;1 antagonist

;

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LA ;2 agonist
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LA ;2 agonist
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Super LA ;2 agonist
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Dobutamine

;1 (;1 cancels out)

x

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