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Notes:
- Buspirone is a
5-HT1A partial agonist.
- It is a full
agonist at the somatodendritic autoreceptors and a partial agonist
at the postsynaptic 5-HT1A receptors. Sussman, 1995:7 (8)
- The reason buspirone
acts as a full agonist in the raphe nuclei was thought to be because
there is a large receptor reserve among autoreceptors in the region,
which would make them more sensitive to buspirone than are the postsynaptic
5-HT1A receptors. This is, however, not the case; full agonists at postsynaptic
receptors have been synthesized.
- Baseline 5-HT
levels and buspirone dose may determine whether the drug produces
an overall agonism or antagonism. Sussman, 1995: 8 (3)
- The major metabolite
of buspirone is 1-(2-pyrimidinyl)-piperazine (1-PP). Sussman, 1995:
8 (7)
- 1-PP acts
as a2-adrenergic antagonist.
- 1-PP does
not bind to dopamine or 5-HT1A receptors.
- Concentrations
of 1-PP in CNS are higher than parent compound.
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