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313 PHL Lab # 3

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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  1. 313 PHLLab # 3 Effect of Certain Agonists & Their Antagonists on The Isolated Rabbit Intestine

  2. 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%)

  3. 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 .

  4. 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) .

  5. 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

  6. Antagonist: Atropine (0.1ml, 0.1%) MOA: It is a reversible, competitive blocker of M3 R.

  7. Design for Determination of site of action of unknown: Blocker + Agonist + Unknown Unknown Agonist

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