Structure-activity relationships Flashcards
(15 cards)
1
Q
What are adrenergic receptors (4)
A
- Involved in the ANS
- Alpha 1 & 2, Beta 1 & 2
- Activating or blocking these G-coupled receptors affects the signalling pathway
- Common drugs treat: hypertension, angina
2
Q
What are beta-blockers (5)
A
- inhibit Beta-1 and beta-2 receptor interactions
- decreased muscle contraction (low heart rate)
- decreased bronchodilation (closes airway)
- widely prescribed class of anti-hypertensives
- first line of treatment for glaucoma
- Majority are aryloxypropanolamines
3
Q
Propanol is a non-selective beta-blocker prescribed for hypertension and anxiety. What side effects might there be? (2)
A
- Non-selective so inhibits Beta-1 and Beta-2 causing vasocontriction in the lung - contraindicated for asthma and bronchitis
- blocking B1 & B2 can indirectly cause vasoconstriction by allowing alpha effects (vasoconstriction) to dominate.
4
Q
What are key features needed for beta-blocker activity (4)
A
- aromatic ring
- ester linkage
- hydroxyl (OH) (secondary alcohol)
- NH (secondary or tertiary amine)
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, some selective have bulkier alkyl groups on amine nitrogen
6
Q
What are adrenoceptors (4)
A
- Stimulating alpha-1 adrenoceptors
- vasoconstriction (increased blood pressure)
muscle contraction in the bronchi (closing the airways) - induce hypertension by stimulating alpha-1 adrenoceptors, causing vasoconstriction (increased blood pressure) in patients in shock
- The structure allowing the molecule to act as an adrenoreceptor agonist is the OH(s) bonded to the aromatic ring
7
Q
What are examples of alpha-1 agonists (3)
A
- Dopamine
- Noradrenaline
- Adrenaline
8
Q
What is the structure of Dopamine (4)
A
- Aromatic ring
- 2x OH at end of aromatic ring
- Carbon chain
- NH₂
9
Q
What is the structure of Noradrenaline (5)
A
- Aromatic ring
- 2x OH at end of aromatic ring
- Carbon chain
- OH
- NH₂
10
Q
What is the structure of Adrenaline (6)
A
- Aromatic ring
- 2x OH at end of aromatic ring
- Carbon chain
- OH
- NH
- CH₃
11
Q
What is phenylephrine (2)
A
- Phenylephrine is used in cold and flu medicine to stop your nose running
- It acts as an α1 agonist causing vasoconstriction
12
Q
What is the structure of phenylephrine (6)
A
- Aromatic ring
- x1 OH at end of aromatic ring
- Carbon chain
- OH
- NH
- CH₃
13
Q
What does activating alpha-1 receptors do (3)
A
- Muscle contraction
- Vasoconstriction
- Increase blood pressure
14
Q
What does activating beta-1 receptors do (2)
A
- Muscle contraction
- Increase heart rate
15
Q
What does activating beta-2 receptors do (2)
A
- Bronchodilation
- Vasodilation
