Korneev A Ia, Faktor M I, Chan T B
Biull Eksp Biol Med. 1988 Jan;105(1):41-3.
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.
在人皮质和海马膜制剂中，丁螺环酮和Mj 138 - 05（浓度高达0.1 mM）不会特异性取代与(3H)色胺、(3H)士的宁、(3H)氟硝西泮和(3H)丙咪嗪结合的物质。同时，这两种化合物对人皮质和海马中(125I)-麦角酸二乙酰胺（LSD）特异性结合位点表现出与5-羟色胺相似的亲和力（IC50在2 - 6 microM范围内）。在海马中，5-羟色胺、丁螺环酮和Mj 138 - 05对(3H) LSD（2 nM）特异性结合位点的IC50分别测定为0.14 microM、2.3 microM和6.1 microM；对海马中(3H) 5-羟色胺特异性结合位点的IC50分别为0.005 microM、3.8 microM和21 microM。5-羟色胺对人皮质(3H) LSD结合位点的亲和力比对海马低10倍，丁螺环酮和Mj 138 - 05对人皮质(3H) LSD结合位点的亲和力比对海马低4倍。然而，5-羟色胺对皮质中(3H) 5-羟色胺结合位点的亲和力与对海马中的相同，而丁螺环酮和Mj 138 - 05对皮质中(3H) 5-羟色胺结合位点的亲和力比对海马低12 - 15倍。得出的结论是，在人脑中，丁螺环酮和Mj 138 - 05以微摩尔亲和力与5-HT2相互作用，并能够与海马中的5-HT1受体亚群结合。
