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Neurotransmitters Safeya Effat
Neurotransmitters Safeya Effat
Neurotransmitters Safeya Effat
1. serotonin
2. norepinephrine
3. dopamine
4. acetylcholine
5. glutamate
6. GABA (ã-aminobutyric acid)
Reuptake systems:
Neurohormones
o A neurohormone is distinguished by the fact that it is released into
the bloodstream rather than into the extraneuronal space in the
brain.
o Once in the bloodstream, the neurohormone can then diffuse into
the extraneuronal space and have its effects on neurons.
Dopamine
Dopamine Receptors
The five subtypes of dopamine receptors can be put into two groups.
1. In the first group, the D1 and D5 receptors stimulate the formulation
of cAMP by activating the stimulatory G protein, Gs.
The D5 receptor has only recently been discovered, and less is known
about it than about the D1 receptor.
One difference between these two receptors is that the D5 receptor has a
much higher affinity for dopamine than does the D1 receptor.
Serotonin
Serotonergic Receptors
Seven types of serotonin receptors are now recognized: 5-HT1 through 5-
HT7, with numerous subtypes, totaling 14 distinct receptors.
The diversity of serotonin receptors has initiated a significant effort to
study the distribution of serotonin receptor subtypes in pathological states
and to design subtype-specific drugs that may be of particular therapeutic
benefit in specific conditions.
For example, buspirone (BuSpar), a clinically effective anxiolytic, is a
potent 5-HT1A agonist, and other 5-HT1A agonists are being developed
for the treatment of anxiety and depression.
The distributed serotonin receptors are sometimes responsible for the side
effects of serotonergic drugs, many of which nonspecifically raise
serotonin levels and thus indiscriminately increase receptor activation.
Histamine
Neurons that release histamine as their neurotransmitter are located in the
hypothalamus and project to the cerebral cortex, the limbic system, and
the thalamus.
Histamine receptors:
H1-receptor stimulation increases the production of IP3 and DAG;
H2 stimulation increases the production of cAMP; and the
H3 receptor may regulate vascular tone.
Blockade of H1 receptors is the mechanism of action for allergy
medications and is partly the mechanism for commonly observed side
effects (e.g., sedation, weight gain, and hypotension) of some
psychotropic drugs.
Acetylcholine
Cholinergic Receptors
The two major subtypes of cholinergic receptors are muscarinic and
nicotinic.
There are five recognized types of muscarinic receptors with various
effects on phosphoinositol turnover, cAMP and cGMP production, and
potassium ion channel activity.
Muscarinic receptors are antagonized by atropine and by the
anticholinergic drugs.
The nicotinic receptors are ligand-gated ion channels that have the
receptor site directly on the ion channel itself.
The nicotinic receptor is actually made up of four subunits (α, β, γ, and
δ). Nicotinic receptors can vary in the number of each of those subunits;
thus, a multitude of subtypes of nicotinic receptors exist, based on the
specific configuration of the subunits.
Glycine
Glycine is synthesized primarily from serine by the actions of serine
trans-hydroxymethylase and β-glycerate dehydrogenase, both of which
are rate limiting.
Glycine does double duty as a mandatory adjunctive neurotransmitter for
glutamate activity and an independent inhibitory neurotransmitter at its
own receptors. The excitatory amino acid-binding site for glycine on the
NMDA glutamate receptor is referred to as the non“strychnine-sensitive
glycine receptor, and it contrasts with the strychnine-sensitive glycine
receptor, which is an inhibitory receptor. Improvement of NMDA
receptor activity by occupancy of the glycine-binding site has been
hypothesized to present an adjunctive mode for the treatment of
schizophrenia. Some, but not all, clinical trials of this hypothesis have
shown a reduction in the negative symptoms of schizophrenia by glycine.
Glutamate
Glutamate is synthesized from glucose and glutamine in presynaptic
neuron terminals and is stored in synaptic vesicles. Once released into the
synaptic cleft, it acts on receptors, and its action is terminated by highly
efficient uptake into the presynaptic neuron or adjacent glia.
Glutamate is the primary neurotransmitter in cerebellar granule cells, the
striatum, the cells of the hippocampal molecular layer and entorhinal
cortex, the pyramidal cells of the cortex, and the thalamocortical and
corticostriatal projections.
Glutamate release is stimulated by nicotine.
Of the five major types of glutamate receptors, the NMDA receptor is the
best understood and most complex of the receptors, because it may play
an essential role in learning and memory, as well as psychopathology.