[Interaction of the anxiolytic agent buspirone with serotonin and other synaptic receptors in the human brain].
Buspirone and Mj 138-05 (up to 0.1 mM) did not displace specifically bound (3H) tryptamine, (3H) strychnine, (3H) flunitrazepam and (3H) imipramine in human cortical and hippocampal membrane preparations. At the same time both compounds displayed similar to serotonin affinity (IC50 in the range of 2-6 microM) for (125I)-LSD specific binding sites in the human cortex and hippocamp. IC50 of serotonin and buspirone and Mj 138-05 for (3H) LSD (2 nM) specific binding sites in the hippocamp was determined as 0.14 microM, 2.3 microM and 6.1 microM, respectively; and for (3H) serotonin specific binding sites in the hippocamp as 0.005 microM, 3.8 microM and 21 microM, respectively. The affinity for human cortex (3H) LSD binding sites was 10-fold lower in case of serotonin and 4-fold lower in case of buspirone and Mj 138-05 than in the hippocamp. However, the affinity for (3H) serotonin binding sites in the cortex was the same as in the hippocamp in case of serotonin and 12-15-fold lower than in the hippocamp in case of buspirone and Mj 138-05. It is concluded that in human brain buspirone and Mj 138-05 interact with micromolar affinity with 5 HT2 and are capable of binding to a subpopulation of 5 HT1 receptors in the hippocamp.
D000368:Aged; D000369:Aged, 80 and over; D014151:Anti-Anxiety Agents / Q000378:metabolism; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002065:Buspirone / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism; D005260:Female; D005445:Flunitrazepam / Q000378:metabolism; D006624:Hippocampus / Q000378:metabolism; D006801:Humans; D007099:Imipramine / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D008875:Middle Aged; D011743:Pyrimidines / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000378:metabolism*; D013331:Strychnine / Q000378:metabolism; D014363:Tryptamines / Q000378:metabolism
D014151:Anti-Anxiety Agents; D011743:Pyrimidines; D017981:Receptors, Neurotransmitter; D011985:Receptors, Serotonin; D014363:Tryptamines; C030820:tryptamine; D005445:Flunitrazepam; D013331:Strychnine; C039979:gepirone; D007099:Imipramine; D002065:Buspirone
Vzaimodeĭstvie anksioloticheskogo agenta--buspirona s serotoninovymi i drugimi sinapticheskimi retseptorami mozga cheloveka.