313 phl lab 3
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313 PHL Lab # 3. Effect of Certain Agonists & Their Antagonists on The Isolated Rabbit Intestine. Effect of stimulant drugs (spasmogens)and their blocker :. 1-Drugs act on neuronal nicotinic (Nn) Receptors: Agonist Dil. Nicotine (0.01%, 0.1ml) Antagonist : Conc. Nicotine (0.1%, 0.1ml)

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313 PHL Lab # 3

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313 phl lab 3

313 PHLLab # 3

Effect of Certain Agonists & Their Antagonists on The Isolated Rabbit Intestine


Effect of stimulant drugs spasmogens and their blocker

Effect of stimulant drugs (spasmogens)and their blocker:

  • 1-Drugs act on neuronal nicotinic (Nn) Receptors:

    Agonist

    Dil. Nicotine (0.01%, 0.1ml)

    Antagonist :

    Conc. Nicotine (0.1%, 0.1ml)

  • 2-Drugs act on muscarinic (M3) Receptors:

    Agonist

    Ach (0.01%, 0.1ml)

    Antagonist :

    Atropine (0.1ml, 0.1%)


1 drugs act on neuronal nicotinic nn receptors

1-Drugs act on neuronal nicotinic (Nn) Receptors:

Agonist

Dil. Nicotine (0.01%, 0.1ml)

MOA:

Dil. Nicotine act on Nn receptor

→ activates Na+-K+ channels

→ rapid ↑ intracellular Na +

→ rapid depolarization

→ increase contraction .


313 phl lab 3

Antagonist :

Conc. Nicotine (0.1%, 0.1ml)

- Conc. Nicotine is depolarizing ganglionic blocker

MOA:

It causes an initial increase in amplitude due to its initial depolarization (↑contraction)

→ Followed by successive depolarization

→ transmission failure & muscular fatigue (blocker of the receptors) .


2 drugs act on muscarinic m3 receptors

2-Drugs act on muscarinic (M3) Receptors:

Agonist :

Ach (0.01%, 0.1ml)

MOA :

Ach stimulates M3R

→ ++ Phospholipase C

→Hydrolysis of (PIP2) into:

1-DAG→ opening of Calcium channels → Ca++ influx → contraction

2- IP3→ mobilization of ca++ from its stores

↑ intracellular calcium →contraction


313 phl lab 3

Antagonist:

Atropine (0.1ml, 0.1%)

MOA:

It is a reversible, competitive blocker of M3 R.


Design for determination of site of action of unknown

Design for Determination of site of action of unknown:

Blocker

+

Agonist

+

Unknown

Unknown

Agonist


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