Studies of the biochemical basis for the discriminative properties of 8-hydroxy-2-(di-n-propylamino)tetralin
作者： Richard A. Rabin , J.C. Winter
DOI: 10.1016/0014-2999(93)90142-5
关键词: Rauwolscine 、 Indorenate 、 Tandospirone 、 Internal medicine 、 Cyclase activity 、 Eltoprazine 、 Gepirone 、 Ipsapirone 、 Flesinoxan 、 Chemistry 、 Endocrinology 、 Pharmacology
摘要: The ability of a series compounds to mimic the stimulus properties 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) was compared to: (1) affinity these for 5-HT1A receptor; and (2) their efficacy inhibit forskolin-stimulated adenylate cyclase activity. Although nine (flesinoxan, MDL 73005EF, gepirone, ipsapirone, buspirone, tandospirone, yohimbine, L 657,743 rauwolscine) complete cross generalization associated with high receptor, eltoprazine, d-lysergic acid diethylamide BMY 7378 had pKD > 7.44, but did not show mimicry 8-OH-DPAT. In addition, indorenate 7.88, yet behavioral response indistinguishable from saline control. Because above data indicated that receptor necessary, sufficient ligand 8-OH-DPAT, in vitro various at determined by measuring inhibition activity hippocampal membranes. For drugs (gepirone, flesinoxan, significant observed, same showed generalization. However, 14802 73005EF alter activity, completely mimicked Eltoprazine inhibiting only 30% responses following administration this drug were on 8-OH-DPAT-appropriate lever. Furthermore, although inhibited compound control.(ABSTRACT TRUNCATED AT 250 WORDS)
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