MD3

1
MD3

• Medicines that send messages to nerves

2
Noradrenaline is released from nerve ends when we
get scared or excited.
3
Noradrenaline binds to receptor molecules and
causes

• Blood pressure increased
• Heart rate increased
• Bronchioles( airways in the lungs) widened
• Sweating increased.

4
Noradrenaline has the structure
primary amine
phenol
phenol
Secondary alcohol
Name 3 functional groups.
5
Asthma affect about 5 of the population. The
airways in the lungs become narrow and inflamed
and filled with mucus. This makes the sufferer
breathless.
6
Noradrenalin is the lead compound having some of
the right effect but also unacceptable side
effects
It widens the bronchioles but causes increased
blood pressure, heart rate and sweating.
Isoprenaline was used for many years but still
affects the heart.
Salbutamol was developed which is more selective.
7
isoprenaline
salbutamol
What are the differences from noradrenaline ?
Secondary amine group
Primary alcohol
8
isoprenaline
salbutamol
The enantiomer of salbutamol is 68 times less
effective. Suggest a reason for this ?
The receptor molecule is chiral so one isomer
fits better.
9
The Pharmacophore is the group of atoms required
for pharmacological activity.
Draw the pharmacophore for Bronchial Dilation.
10
A compound that contains the pharmacophore will
act on the receptor.
It is called an Agonist
A compound that contains only part of the
pharmacophore will bind to the receptor but not
trigger the response. It will block the bodys
neurotransmitters from binding.
It is called an Antagonist
11
Propranolol is a noradrenaline antagonist.
It blocks the ß-receptors that control heart
muscles.
What are the differences that prevent it
triggering as response?