[An analysis of the hypothermic action of 8-hydroxy-2-(di-N-propylamino)tetralin, 1-(2-pyrimidinyl)piperazine and its derivatives].
The hypothermic activity of 8-OH-DRAT, 1-(2-pyrimidinyl) piperazine (1-PP), buspirone and its structure analogues tightly correlates with the degree of inhibition of 3H-serotonine release by electrically stimulated dorsal raphe slices (r = 0.84), but not cerebral cortex slices (r = 0.66). The pretreatment of mice with p-chlorphenylalanine decreased the hypothermic effects evoked by 8-OH-DRAT, buspirone, campirone (but not 1-PP) only in first 30 min after there injection. It was concluded that hypothermic effects of 8-OH-DRAT, buspirone and its structure analogues were bound with preferable influence as partial agonists on the postsynaptic serotonine 1A receptors. Ipsapirone as a partial agonist has maximal antagonistic activity.
Komissarov
I V
IV
Dolzhenko
A T
AT
Obraztsova
O G
OG
Zin'kovskaia
L Ia
LIa
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D002065:Buspirone / Q000031:analogs & derivatives* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D010134:Fenclonine / Q000494:pharmacology; D007035:Hypothermia / Q000139:chemically induced*; D051379:Mice; D009281:Naphthalenes / Q000494:pharmacology*; D051381:Rats; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D013997:Time Factors
D009281:Naphthalenes; D012702:Serotonin Antagonists; D013764:Tetrahydronaphthalenes; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; C037921:1-(2-pyrimidinyl)piperazine; D010134:Fenclonine; D002065:Buspirone
Analiz gipotermicheskogo deĭstviia 8-oksi-2-(di-N-propilamino)--tetralina, 1-(2-pirimidinil)--piperazina i ego proizvodnykh.