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Explore the development of designer medicines that communicate with nerves, focusing on the key neurotransmitters Noradrenaline and Isoprenaline to treat conditions like asthma. Dive deep into pharmacore and understand the crucial roles of agonists and antagonists in medication efficacy.
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Storyline MD3 Medicines that send messages to nerves.
Designer medicines • Need a biological understanding of the disease • Need a lead compound – provides a lead / gives some clues.
Adrenal gland Flight Fight • Adrenaline • Increases blood pressure • Increases heart rate • Dilates bronchioles
NORADRENALINE • NEUROTRANSMITTER • Fits into and interacts with receptor sites so: • Increases blood pressure • Increases heart rate • Dilates bronchioles • Increases sweating
ISOPRENALENE • AGONIST • Fits into and interacts with 3 receptor sites so: • Increases blood pressure • Increases heart rate • Dilates bronchioles • NORADRENALINE • NEUROTRANSMITTER • Fits into and interacts with receptor sites so: • Increases blood pressure • Increases heart rate • Dilates bronchioles • Increases sweating Can be dangerous!
SALBUTAMOL • AGONIST • Selective – only fits into one receptor site. • Dilates bronchioles. Also CH2OH slows down breakdown.
SALMETEROL AGONIST Longer lasting protection
Pharmocore – group of atoms which make the molecule pharmacologically active.
The structural fragment which is the pharmocophore has: • A shape which precisely fits that of the receptor site • Functional groups which are correctly positioned to interact with the receptor site. • This is called molecular recognition.
Are they all the same colour? chromophore
Agonists and antagonists Salbutomol is an agonist – behave like a natural substance from the body.