531 - Med Chem I - Exam Iii - Histamine

Front 1

What are some of the main functions of histamine?

Back 1

Mediate allergic inflammatory response, and regulate secretion of gastric acid

Front 2

Where are H1 receptors located and what are their main functions?

Back 2

Located peripherally and also in the CNS; stimulates contraction of smooth muscles in the gut, uterus and bronchi

Front 3

Where are H2 receptors located and what are their main functions?

Back 3

Located at postsynaptic receptor in parietal cells that secrete acid.

Front 4

Where are H3 receptors located and what are their main functions?

Back 4

Located at presynaptic receptor pin the CNS; antagonists are in clinical trials (sleep disorders, cognitive disfunction , pain and obesity)

Front 5

What is the main purpose of H1 antagonists?

Back 5

Block unwanted effects on smooth muscle of histamine release

Front 6

What is the main purpose of H2 antagonists?

Back 6

Block histamine-induced cascade leading to increased secretion of gastric acid; treat gastric ulcers

Front 7

What is the main difference between first generation and second generation H1 antagonists that leads to a difference in side effect profile?

Back 7

Second generation can't cross the BBB.

Front 8

What is the active tautomer of histamine?

Back 8

N-tau-H tautomer of monocation

Front 9

What are the different classes of first generation H1 antagonists?

Back 9

ethylenediamines, ethanolamines, piperazines, alkylamines and tricyclics

Front 10

What are the two main classes of drugs used to treat gastric ulcers?

Back 10

Proton-pump inhibitors (ATPase inhibitors) and H2 antagonists

Front 11

What special type of inhibitor is omeprazole?

Back 11

Mechanism-based inhibitor