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Psychopharmacology > 3 - Neurotransmission > Flashcards

3 - Neurotransmission Flashcards

1
Q

Allosteric modulators only modify the effects of __. When given alone they have __ ___.

A

Agonists | no effect

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2
Q

Allosteric Modulators (3 points)

A
  • Only modify effects of an agonist and have no effect when given alone.
  • Often have greater receptor subtype selectivity than agonists or antagonists.
  • Modulators of metabotropic receptors may result in better drugs to treat psychiatric and neurological disorders
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3
Q
  1. Many Ionotropic and Metabotropic Receptors have additional binding sites called __ __
  2. Molecules, such as drugs, that bind to such sites and alter functioning of the receptor are called __ __ and can have a positive or a negative effect on receptor signaling
A

Allosteric Sites | Allosteric Modulators

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4
Q

Some proteins involved in exocytosis are targets for drugs or toxins. __ blocks transmitter release at neuromuscular junctions, causing paralysis. Enzymes in the toxin attack proteins involved in exocytosis

A

Botulism (a bacterial toxin)

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5
Q

Stimulates protein kinase A (PKA).

A

Cyclic Adenosine Monophosphate (cAMP)

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6
Q

Regulated by the gas NO; stimulates protein kinase G (PKG).

A

Cyclic Guanosine Monophosphate (cGMP)

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7
Q

__ __ are important locations for synapses to form

A

Dendritic Spines

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8
Q

Ca2+ binds to receptors and results in fusion of vesicle membranes with the cell membrane, releasing neurotransmitter molecules into the synaptic cleft

A

Exocytosis

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9
Q

G proteins act in two ways

A
  • Inhibit or Activate ion channels (ex: K+ channels open, K+ moves out of cell and hyperpolarization results).
  • Stimulate or inhibit Effector Enzymes in cell membrane to synthesize or break down 2nd messenger molecules
    • The neurotransmitter molecule is the first messenger.
    • 2nd messenger is molecule inside cell that carries out biochemical change signaled by first messenger.
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10
Q
  1. Consist of 4 or 5 subunits with an ion channel in center
  2. When transmitter binds to the ___ the channel opens and allows ion flow. This is a __-__ __ __
  3. __ occurs when channel remains closed despite ligands bound to receptor
  4. Some __ __ are Na+ channels; result is __ and an __ __ (nicotinic receptor for ACh).
  5. Others allow Na+ and Ca2+ flow. Ca2+ can act as __ __.
  6. Others allow flow of Cl–, leading to __ (__ __)
A
  1. Ionotropic Receptors
  2. Receptor | Ligand-Gated Channel Receptor’
  3. Desensitization
  4. Ionotropic Receptors | Depolarization and an Excitatory Response
  5. Second Messenger
  6. Hyperpolarization (inhibitory Response)
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11
Q

There are two major categories of transmitter receptors

A

Ionotropic and Metabotropic

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12
Q

Enzymes that transfer a phosphoryl group from a nucleoside triphosphate (ex: Adenosine TriPhosphate)

A

Kinases

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13
Q

These receptors

  • act more slowly, but the response lasts longer.
  • consist of one subunit, with 7 transmembrane domains (7-TM receptors).
  • work by activating G proteins (G protein- coupled receptors).
A

Metabotropic receptors

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14
Q

__ __ __ must be packaged into large vesicles in the cell body, so recycling of these vesicles cannot occur at the axon terminal

A

Neuropeptide Precursor Proteins

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15
Q

Neurotransmitter release is regulated by

A
  • rate of neuron firing
  • the probability that vesicles will undergo exocytosis;
  • autoreceptors
    • reduce the amount of transmitter released;
    • they are receptors for same transmitter released by neuron. (e.g., thermostat)
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16
Q
  1. Neurotrasmitter synthesized and stored in vesicles.
  2. A wave of depolarization reaches the axon terminals
  3. Depolarization of presynaptic terminal causes
  4. Voltage-gated Ca2+ channels to open and Ca2+ rushes into the cell
  5. Ca2+ causes vesicles to fuse (dock) with presynaptic membrane in the active zone and are primed for release. Various proteins involved.
  6. Neurotransmitter released into synpatic cleft via Exocytosis
  7. NT binds to receptor molecules in postsynpatic membrance causing…
  8. opening or closing of postsynaptic channels
  9. Postsynaptic current causes excitatory or inhibitory postsunaptic potential that changes exitability of postsynaptic cell
  10. The vesicle membrane is recycled by endocytosis—the cell membrane buds and pinches off a portion, which then fuses with an endosome.
A
  • Many proteins are involved in exocytosis and vesicle recycling.
    • ​Clathrin coats membrane & initiates invagination/vesicle retrieval
    • Synaptobrevin helps vesicle fuse with axon terminal membrane - its the most abundant protein found in synpatic vesicles.
17
Q

Many neurotransmitters have signaling functions outside the CNS, such as __ __ (__), and __ (__)

A

Nitric Oxide (NO), and Acetylcholine (ACh)

18
Q
  1. Breaks down a phospholipid in cell membrane and liberates two 2nd messengers, ___ and ___
  2. Together they cause increase in Ca2+ ions in postsynaptic cell and ativation of __ __ __
  3. Ca2+ acts as a 2nd messenger, but activation of protein kinase requires participation of another protein called __
A
  1. Phosphoinositide | Diacylglycerol (DAG) | Inositol trisphosphate (IP3)
  2. protein kinase C (PKC)
  3. calmodulin — calcium/calmodulin kinase (CaMK).
19
Q

Area of the dendritic membrane facing the synaptic cleft with many neurotransmitter receptors

A

Postsynaptic Density

20
Q

Neurotransmitters bind to more than one type of receptor because there are __

Drugs can be designed to affect specific __ __ which can result in fewer side effects.

A

Subtypes | Receptor Subtypes

21
Q

Receptors are not __. Their role is to pass a signal to the __ __

After binding to a receptor and activating it the transmitter disengages and is free to __, __, or __

A

Transporters | Pass a Signal | Postsynaptic Cell

bind to another receptor | be inactivated | be reabsorbed.

22
Q

Recycling mechanisms occur only with small vesicles containing __ __

A

Classical Transmitters

23
Q
  1. __ __ are molecules inside the cell that activate protein kinases to cause __ of substrate proteins
  2. The added __ groups alter the function of the protein
  3. Phosphorylation of nuclear proteins can __ __/__ __ __
A
  1. Second Messengers | Phosphorylation
  2. Phosphate
  3. Turn on/off gene expression
24
Q

To stop signal transmission, the neurotransmitter molecules must be removed from the synaptic cleft (3 ways)

A
  • Transmitter may be broken down by enzymes — common for ACh, lipid and gaseous transmitters, and neuropeptides
  • Reuptake — transmitters are taken up by the cell that released them.
    • Transporter proteins in cell membrane take up transmitter molecules (important for amino acid transmitters).
  • Transmitters may be taken up by the postsynaptic cell or astrocytes
25
Q

__ __ form the basis of almost all actions of psychoactive drugs

They work by a variety of mechanisms:

A

Synaptic Effects

  • Block storage of NT in synaptic vesicles (making less available):
    • Reserpine (for hypertension) blocks storage of DA, NE, and 5-HT in vesicles.
  • Can stimulate release of NT by reversing action of uptake transporters:
    • Amphetamine stimulates release of DA and NE; fenfluramine stimulates release of 5-HT.
  • Can stimulate or inhibit autoreceptors:
    • Clonidine and 8-OH-DPAT stimulate autoreceptors for NE and 5-HT, reduce NT release
    • ​​pindolol inhibits 5-HT autoreceptors, increases NT release
  • Can act on postsynaptic receptors
    • Agonist: Mimics NT effect on receptor.
      • Benzodiazepines, heroin, morphine, nicotine, THC
    • Antagonist: Inhibits effect of NT on the receptor.
      • Caffeine; antagonists of D2 receptor used to treat schizophrenia
26
Q

Helps the vesicle fuse with the axon terminal membrane. It is the most abundant protein found in synaptic vessicles.

A

Synaptobrevin

27
Q

Triptophan crosses the __ __ __ and turns in to __ in the brain, which converts then to __

A

Blood Brain Barrier | Seratonin | Melatonin

28
Q
  1. Drugs can __ or __ autoreceptors
  2. Drugs can block storage of __ in __ __, making less available
  3. Reserpine blocks storage of __, __, and __ in vesicles
  4. Clonidine and 8-OH-DPAT stimulate autoreceptors for __ and __, reducing release of neurotransmitters
A
  1. stimulate | inhibit
  2. Neurotransmitters | Synaptic Vesicles
  3. DA | NE | 5-HT
  4. NE | 5-HT

Psychopharmacology (14 decks)

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