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The pharmacological properties of a novel selective 5-hydroxytryptamine1A (5-HT1A) receptor antagonist, NAD-299 [(R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate] were examined in vitro and in vivo and compared with the reference 5-HT1A receptor antagonist, WAY-100635(More)
In the search for new 5-hydroxytryptamine (5-HT) receptor antagonists it was found that the compound (R)-(+)-2-[[[3-(morpholinomethyl)-2H-chromen-8-yl]oxy] methyl] morpholine methanesulfonate, (R)-25, is a selective rat 5-hydroxytryptamine1B (r5-HT1B) receptor antagonist. The binding profile showed a 13-fold preference for r5-HT1B (Ki = 47 +/- 5 nM; n = 3)(More)
The effects of repeated treatment of rats with 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), 1.0 mg/kg, subcutaneously, twice daily for 7 days, on the stimulation of post- and presynaptic 5-HT1A receptors were examined. The postsynaptic responses, hypothermia and inhibition of the cage-leaving response, evoked by 0.05 mg/kg 8-OH-DPAT, were measured 48(More)
The effect of the non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists dizocilpine and phenycyclidine, the competitive NMDA antagonist 3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPP) and the antagonist at the glycine modulatory site of the NMDA receptor, 3-amino-1-hydroxy-2-pyrrolidone (HA-966) on the long lasting attenuation of some(More)
The ejaculatory response following acute injections of p-chloroamphetamine (PCA) and several other drugs was measured by weighing the compact seminal material accumulated over 2 hr. p-Chloroamphetamine caused a dose-dependent ejaculatory response that was inhibited by the inhibitor of the synthesis of 5-hydroxytryptamine (5-HT), p-chlorophenylalanine(More)
A practical spatio-temporal database (STDB) technique for dynamic urban land management is presented. One of the STDB models, the expanded model of Base State with Amendments (BSA), is selected as the basis for developing the dynamic cadastral management technique. Two approaches, the Section Fast Indexing (SFI) and the Storage Factors of Variable(More)
The biochemical and behavioural effects of isamoltane, a beta-adrenoceptor and 5-HT1B receptor antagonist that has higher affinity for 5-HT1B receptors than for 5-HT1A receptors, on 5-HT neurotransmission in the rat brain were examined. In binding experiments isamoltane was found to be about five times more potent as a ligand for the 5-HT1B receptor than(More)
The effects of acute doses of 8-hydroxy 2-(di-n-dipropylamino)tetralin (8-OH-DPAT) on the hypothermic response, induced by a challenge dose of 8-OH-DPAT, were examined in rats. Acute doses of 8-OH-DPAT (1.0 or 0.5 mg/kg, s.c.) significantly attenuated the hypothermic response induced by 8-OH-DPAT (0.05 mg/kg, s.c.). The response to 8-OH-DPAT was almost(More)
  • L Rényi
  • 1986
The effects of the depletion of 5-hydroxytryptamine (5-HT) in the rat brain upon the 5-HT behavioural syndrome (ejaculatory response, abduction of hind-limbs, forepaw treading, and Straub tail) induced by 5-methoxy-N,N-dimethyltryptamine (1 mg/kg intraperitoneally) were investigated. The 5-HT depletion was produced by p-chlorophenylalanine (PCPA 2 X 200(More)