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• W2072135567 abstract "In combined biochemical and functional studies it has been possible to show that ergocornine (0.5–5 mg/kg) and the ergolene derivative (5R,8R)-8-(4-p-methoxyphenyl-1-piperazinylmethyl)-6-methylergolene (PTR 17402; MPME) (0.25–5 mg/kg) reduce in a dose-dependent way brain 5-hydroxytryptamine (5-HT) turnover in rat as evaluated with tryptophan hydroxylase inhibitor, α-propyl-dopacetamide (H 22/54), whereas 2-Br-α-ergocryptine (CB 154; Br-EC) had no effect on brain 5-HT turnover. Effects on 5-HT receptors activity were evaluated using the extensor hindlimb reflex of acutely spinalized rats. It was found that ergocornine increased the 5-HT receptor activity independent of presynaptic 5-HT stores and that it did not have any effects on uptake retention and spontaneous overflow of 3H-5-HT in vitro but reduced the field stimulation-induced release 3H-5-HT in vitro. Therefore, it is suggested that ergoconine is a 5-HT receptor-stimulating agent, an effect which may lead to reduction of nervous impulse flow in the 5-HT neurons and subsequently of 5-HT release and turnover. MPME, on the other hand, seems to increase 5-HT receptor release of 5-HT stores, mainly from extragranular sites. Thus, the increase in extensor reflex activity found after MPME was reduced by reserpine and H 22/54 and enhanced by nialamide and in vitro MPME markedly increased 3H-5-HT overflow in cortical slices of nialamide-pretreated rats and inhibited uptake and retention of 3H-5-HT (EC50 = 1.6 × 10−6 M) in cortical slices of normal rats. Inhibition of the 5-HT membrane pump does not seem to be of any major importance, since chlorimipramine was only weakly active on the extensor reflex in the pharmacological models used and since MPME did not block but rather enhanced the 5-HT depletion caused by 4-methyl-α-ethyl-m-tyramine. It is suggested that MPME is a releaser of extragranular 5-HT stores leading to increased 5-HT receptor activity and reduction of 5-HT turnover in the same way as indicated for ergocornine. This new ergolene derivative may represent a new class of antidepressant drugs acting via release of extragranular 5-HT stores." @default.
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• W2072135567 date "1975-02-01" @default.
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• W2072135567 title "Effect of ergot drugs on central 5-hydroxytryptamine neurons: Evidence for 5-hydroxytryptamine release or 5-hydroxytryptamine receptor stimulation" @default.
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• W2072135567 doi "https://doi.org/10.1016/0014-2999(75)90097-7" @default.
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