Introduction to structure-activity relationships Flashcards
1
Q
What are adrenergic receptors (5)
A
- An important class of receptors that are involved in the autonomic nervous system
- There are four types of receptors: α1, α2, b1 and b2
- Drugs act to either stimulate the adrenergic system or inhibit it (beta-blockers)
- Activating or blocking this GPCR affects the signalling pathway
- Common drugs treat: hypertension, angina
2
Q
What are beta-blockers (4)
A
- work by inhibiting Beta-1 and beta-2 receptor interactions
- decreased mucscle contration (low heart rate) and decreasng bronchodilation (closes airway)
- anti-hypertensives
- Also, first line of treatment for glaucoma
3
Q
Propranolol is a non-selective beta-blocker what side effects might there be (1)
A
inhibits Beta-1 and Beta-2 causing vasocontriction in the lung - contraindicated for asthma and bronchitis
4
Q
What functional groups are present in beta-blockers (4)
A
- aromatic ring
- ester linkage
- hydroxyl (OH)
- NH
5
Q
What are the structural differences between selective and non-selective beta-blockers (2)
A
- non-selective beta-blockers have a secondary aromatic ring
- selective beta-blockers lack a secondary aromatic ring
6
Q
How do adrenoreceptor agonists work (2)
A
- alpha-1 adrenoceptors = vasoconstriction and muscle contraction in the bronchi
- used to induce hypertention in patients in shock
7
Q
What are the structures allowing molecules to work as a adrenoreceptor agonists (4)
A
- hydroxyl(s) bonded to aromatic ring
- aromatic ring
- terminal NH2
- sometimes OH on hydrocarbon chain
- The structure allowing the molecule to act as a adrenoreceptor agonist is the OH(s) bonded to the aromatic ring
8
Q
What are examples of adrenoreceptor agonists (3)
A
- dopamine
- noradrenaline
- adrenaline
9
Q
What is phenylephrine and what does it do (2)
A
- Phenylephrine is used in cold and flu medicine to stop your nose running
- It acts as an α1 agonist causing vasoconstriction
