Psychopharm Part I Flashcards
Defining properties of neurotransmitters?
1) synthesized and released from neurons; 2) released from nerve terminals in a chemically or pharmacologically identifiable form; 3) interact with postsynaptic receptors and brings about the same effects as are seen with stimulation of the presynaptic neuron; 4) interaction with the postsynaptic receptor displays a specific pharmacology; 5) actions are terminated by active processes
Major receptor subtypes?
- Ionotropic 2. G-protein coupled (GPCRs) 3. Receptor tyrosine kinases 4. Nuclear receptors
Ionotropic receptors
- relatively self-contained in structure - message takes the form of transmembrane ion fluxes
GPCRs
multicomponent in nature and generate intracellular second messengers
receptor tyrosine kinases and phosphatases
contain intrinsic enzymatic activity
Nuclear receptors
- cytoplasmic 2. translocate to the nucleus to directly regulate transcription (gene expression) 3. activated by lipophilic molecules (often hormones) that enter the cell
Autoreceptors
located on neurons that produce the endogenous ligand for that particular receptor (e.g., a serotonergic receptor on a serotonergic neuron)
Heteroreceptors
present on neurons that do not contain an endogenous ligand for that particular receptor subtype (e.g., a seroto-nergic receptor located on a dopaminergic neuron).Definition
Types of autoreceptors
- Somatodendritic (on cell bodies, regulate firing rate of neurons) 2. Nerve terminal (regulate amount of neurotransmitter released per nerve impulse)
What kind of receptor is the glutamate receptor (e.g. NMDA)?
Ionotropic
What kind of receptor is the GABA receptor?
Ionotropic
What kind of receptor is the ACh receptor?
Ionotropic
The 3 modes of regulation of GPCRs?
- Desensitization (homologous and heterologous) 2. Downregulation 3. Trafficking
50% of 5HT neurons are in…
the dorsal raphe
Presynaptic regulation of 5HT is via which receptors?
somatodendritic 5-HT1A and autoreceptors 5-HT1B and 5-HT1D
Which aminoacid is the precursor for 5-HT?
L-Tryptophan
What is the rate-limiting step in the production of serotonin?
Converting from tryptophan to 5-hydroxytryptophan by *tryptophan hydroxylase*
Which enzyme converts 5-hydroxytryptophan to serotonin?
amino acid decarboxylase
What is the metabolite of serotonin?
MAO converts it to 5-HIAA (5-hydroxyindoleacetic acid)
tryptophan depletion triggers depressive relapse in patients treated with ____(1)____ but NOT in those treated with ____(2)_______
1) SSRIs 2)NRIs
5-HT1A receptor is downregulated by…
adrenal steroids but NOT 5-HT
Which autoreceptors are present on the presynaptic terminal of 5HT neurons?
5-HT1B and 5HT1D
The ratio of D2/5-HT2 blockade confers…
atypicality in antipsychotics
5HT2 receptors are downregulated by…
chronic administration of antidepressants
5HT2 receptors are upregulated by…
ECT