SDZ GLC-756, a novel octahydrobenzo[g]quinoline derivative, is equipotent in displacing [3H]SCH23390 from dopamine D1 receptors and [3H]205-501 from dopamine D2 receptor binding sites. It blocks dopamine sensitive adenylate cyclase with the same potency as SCH23390, indicating antagonist properties at dopamine D1 receptors. On the other hand, SDZ GLC 756 inhibits electrically evoked acetylcholine release from rat striatal slices with the same potency as the selective dopamine D2 receptor agonist bromocriptine. This effect is blocked by spiperone suggesting that it is mediated by dopamine D2 receptor activation. The opposing action of SDZ GLC 756 on dopamine D1 and D2 receptors is also evident in vivo. SDZ GLC 756, like SCH23390, blocks apomorphine-induced rearing in mice. On the other hand, it inhibits prolactin secretion and produces circling in unilateral 6-OHDA-lesioned rats, which is compatible with stimulant properties at dopamine D2 receptors. This drug might be a new tool to study linkage between dopamine D1 and D2 receptors.
Remote asynchronous usability testing is characterized by both a spatial and temporal separation of users and evaluators. This has the potential both to reduce practical problems with securing user attendance and to allow direct involvement of users in usability testing. In this paper, we report from an empirical study where we systematically compared three methods for remote asynchronous usability testing: user-reported critical incidents, forum-based online reporting and discussion, and diary-based longitudinal user reporting. In addition, conventional laboratory-based thinkaloud testing was included as a benchmark for the remote methods. The results show that each remote asynchronous method supports identification of a considerable number of usability problems. Although this is only about half of the problems identified with the conventional method, it requires significantly less time. This makes remote asynchronous methods an appealing possibility for usability testing in many software projects.
UV. ‐irradiation of the 11‐oxo‐δ14‐5α‐pregnene derivate 16 gives rise to a novel photochemical reaction. The preferential attack of the photochemically excited carbonyl on CH‐8 furnishes the tertiary cyclopropanol compound 18 in high yield.
CK 204-933 displaces [3H]dopamine and [3H]spiperone with high affinity from D-1 and D-2 recognition sites in membranes of calf caudate. Results from functional in vitro tests suggest that it is a partial agonist at D-1 receptors and an antagonist at D-2 receptors. These opposite effects at dopamine receptor subtypes are also expressed in vivo. For instance, in 6-hydroxydopamine lesioned rats, CK 204-933 induces contralateral rotations which are antagonised by SCH 23390 but not by sulpiride. On the other hand, CK 204-933 induces a long lasting increase of dopamine turnover in rat striatum and antagonises apomorphine-induced gnawing behaviour in rats. CK 204-933 increases prolactin serum levels in rats after subcutaneous administration, whereas after oral administration a moderate decrease of prolactin serum levels was seen. The latter effect is probably due to the formation of active metabolites. CK 204-933 exhibits also a high affinity to [3H]prazosin binding sites and antagonises serotonin-mediated stimulation of adenylate cyclase in rat hippocampus. On the other hand, CK 204-933 has no effect of only very weak effects on noradrenaline and serotonin release from rat cerebral cortex slices, which is consistent with its weak effects on noradrenaline- and serotonin-turnover in rat brain. Based on these properties it is suggested that CK 204-933 could be of therapeutic value in brain diseases associated with disturbances of monoaminergic neurotransmission.
The UV.‐isomerisation of 11‐oxo‐14β,17α‐pregnane 9 to the 11,19‐cyclo‐derivative 11 is described. In addition the Pb(OAc)4‐fragmentation of photoproduct 11 was investigated. 11 yielded besides the expected 11‐oxo‐19‐hydroxy‐pregnane 18 the novel 9,11‐seco‐11,19‐cyclosteroid 19. The structure of 19 was established by chemical transformations and subsequently confirmed by X‐ray analysis [2].
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