Med design

Question 1

what is the rule of 5 for CNS active drugs

Answer 1

• MW< 450
• log P= 0-5 or log D= 1-3 (log D is log P at a certain pH e.g. 7) ‘high’ but within limit
• H-bond= 0-5 (donor H<2)
• PSA= 40-90
• PKa= 8-10 (no acid)
• NO CARBOXYLIC ACID

Question 2

what are the common features for all CNS active compounds?

Answer 2

an aromatic ring system + basic N (normally 2 units apart)

Question 3

why does marijuana increase your appetite?

Answer 3

marijuana contains active constituent of Δ9-THC (dronabinol), a non-selective cannabinoid agonist, bind CB1 rec on pre-syn, inhibitory resp: decrease Ca, 5HT, NA, glu, gaba, appetite stimulant

Question 4

how can you reduce logp (from rimonabant to NIDA-41020)

what prob can it cause?

Answer 4

Reduce the log p by adding O(Me group), then that affects no. of H bond

Question 5

MOR knockout mice display reduced motivation to eat and are resistant to diet-induced obesity, why?

Answer 5

miu opioid rec antagonist reduces the reward feeling you get from eating palatable food, this reduces food intake

Question 6

how does naltrexone work?

Answer 6

naltrexone is an opioid rec inverse agonist, it indirectly modulate activation of reward center e.g. mesolimbic pathway by reducing DA bind to D2 rec. this decreases pleasure you get with food (which high in fat, sugar) consumption
Mor on Gaba to da to nacc

Question 7

What is the stereochemistry of the two chiral centres present in the structure of delta-9-THC and CBD cannabidiol?

Answer 7

both R

Question 8

What is the structure of CB receptors?

Answer 8

7TM GPCR

transmembrane

Question 9

Where are CB1 rec found in neurones?

Answer 9

Pre-synaptic neurones

Question 10

What is the function of CB1?

Answer 10

Retrograde control of release of inhibitory and stimulatory NTs

Question 11

Where is CB2 rec found?

Answer 11

In immune cells

Question 12

What’s the function of CB2

Answer 12

Control the activity and migration of immune cells

Question 13

What is the precursor of endogenous Cannabinoids?

Answer 13

Arachidonic acid in lipid membrane

Question 14

Bupronorphine is

Answer 14

A miu opioid partial agonist
Kappa antagonist
Analgesic
Trt for opioid dependence

Question 15

Salvia is a kappa opioid agonist meaning …

Answer 15

Analgesic but not used due to 
Psychoto mimic effect. 
Loss of body or identity 
Hysteric laughter 
Overlapping realities

Question 16

Similarity of buprenophine and methadone

Answer 16

Mu opioid receptor agonist (bu-partial)
Highly lipophilic
Long duration of action
Minimise withdrawal symptoms