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 Fight Flight 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

Asthma

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 CH 2 OH slows down breakdown.

SALMETEROL AGONIST Longer lasting protection

Do Ass 6 and 7.

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

Solubility?

Agonists and antagonists Salbutomol is an agonist – behave like a natural substance from the body.

Antagonists

Do Ass 8