Chapter 7: Fig 1.15

Question 0

Drugs that bind at the Benzodiazepine receptor site can do one of three things :
Agonists( diazepam ) increase
Antagonists ( Ro 15-1788) increase
Inverse Agonists B-Carbolines) decrease

Answer 0

Agonist: help open GABA to open the Cl channel and extra Cl flows in
Antagonist: block receptor and prevent other BDZs from binding there
Inverse Agonists: reduces the effect of GABA thus causing the Cl- channel to close , preventing the ion from entering the cell.

Question 1

When the Chloride ionophore is opened the release of Cl- cause?

Answer 1

• an inhibitory effect, firing of cell decreases or it becomes more diff to fire via another neuron

Question 2

Agonists will ____ anxiety, antagonists will ____ unless another BDZ is present, and inverse agonists will cause ___. These three types of BDZ will also affect _____ caused naturally or bypentylenetetrazol.

Answer 2

reduce, do nothing, anxiety, seizures

Question 3

Normally it takes ___ mg/kg of pentylenetetrazol (closes Cl channel) to cause a seizure in the avg rat. The BDZ agonist diazepam raises the amount to ___mg/kg. The inverse agonist FG 7142 ___ amount required to ___mg/kg. The antagonist Ro15-1788 has no effect: 70mg/kg which is no different than 65.

Answer 3

-65, 268, lowers, 30

Question 4

Barbiturates on GABA-BZD supramolecular complex

Answer 4

• no limit to open a channel for chloride ions…aka direct

Question 5

Ethanol and GABA-BZD supramolecular complex

Answer 5

directly effects Cl- channel

Question 6

Benzodiazepine and GABA-BZD supramolecular complex ?

Answer 6

has a limit , doesn’t directly affect channel but the GABA receptor which in turn stims Cl channel.

Question 7

Picrotoxin site and GABA-BZD supramolecular complex

Answer 7

direct

Question 8

GABA-BZD supramolecular complex :
Agonists at the GABA-a( Muscimol) , BZD( diazepam) , ethanol (ethanol) , and BAR(pentobarbital) sites all increase chloride ……..but Picrotoxin( pentylenetetrazole) ?

Answer 8

-lowers Cl-

Question 9

Only antagonists at GABA-a(bicuculline) and BZD( Ro 15-1788)

Answer 9

• gaba-a: decreases Cl

- BZD: decreases

Question 10

Inverse Agonists at ethanol ( Ro 15-453) , BZD ( B-carbolines)

Answer 10

-decrease Cl- closing channel

Question 11

Diazepam binding inhibitor at BZD receptor?

Answer 11

-decreases Cl-