WAY-100635 Maleate 1092679-51-0

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Molecular Weight:

538.64 WAY-100635 Maleate is a potent and selective 5-HT1A receptor agonist with pIC50 of 8.87, exhibits >100-fold selectivity against other 5-HT receptor subtypes and major neurotransmitter receptors.

Biological Activity

In dorsal raphe nucleus (DRN) slices superfused with WAY 100635 (10 nM),
the majority of putative 5-HT neurons increase their firing rate (13%
of baseline rate). In addition, WAY 100635 completely prevents the
decrease in firing rate produced by 5-HT (3-15 μM), 8-OH-DPAT (10 nM),
5-carboxamidotryptamine (20 nM) and lesopitron (100 nM).

The antagonism
exerted by WAY 100635 is fully surmounted by increasing the
concentration of 5-HT to 300 μM with an IC50 of 0.95 nM. In hippocampal
slices, WAY 100635 (0.5 nM -10 nM) does not alter the resting membrane
potential or the membrane input resistance of intracellularly recorded
CA1 pyramidal cells. However, WAY 100635 completely prevents not only
the hyperpolarization, with an IC50 of 1.3 nM, but also the decrease in
membrane input resistance produced by 5-HT and 5-carboxamidotryptamine
with IC50 of 22.5 μM and 50 nM, respectively.

WAY 100635
has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A
site relative to a range of Other CNS receptors. The Bmax of [3H]WAY 100635 specific binding is consistently 50-60% greater than that of the agonist radioligand, [3H]8-OH-DPAT. Mn2+, but not guanine nucleotides, inhibits [3H]WAY
100635-specific binding.

WAY 100635 has no 5-HT1A receptor agonist
actions, but dose-dependently blocks the effects of agonists at both the
postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus, and
the somatodendritic 5-HT1A receptor locates on dorsal raphe 5-HT
neurones. [3H]WAY 100635 has a Kd of approximately 2.5 nM.

In the isolated guinea-pig ileum WAY 100635 is a potent and, at high
concentrations, an insurmountable antagonist of the 5-HT1A receptor
agonist action of 5-carboxamidotryptamine, with an apparent pA2 value
(at 0.3 nM) of 9.71. Five minutes after the i.v. injection of [3H]WAY
100635 (4 μCi -7.6 μCi per mouse) the amount of tritium found in the
whole brain only accounted for 1.5-1.8% of the injected radioactivity,
regional differences in 3H accumulation already correspondes to those of 5-HT1A receptor density. In light of its only recently discovered dopaminergic activity,
conclusions drawn from studies that employs WAY 100635 as a selective
5-HT1A antagonist may need to be re-evaluated.


[3H]WAY 100635 is shown to bind selectively to brain 5-HT1A
receptors, following intravenous administration to mice. WAY 100635 also
dose-dependently blocks the ability of 8-OH-DPAT to inhibit the firing
of dorsal raphe 5-HT neurones, and to induce the '5-HT syndrome',
hypothermia, hyperphagia and to elevate plasma ACTH levels.

In the mouse
light/dark box anxiety model, WAY 100635 induces anxiolytic-like
effects. WAY 100635 has no intrinsic effect on cognition in the
delayed-matching-to-position model of short-term memory in the rat, but
reverses the disruptive effects of 8-OH-DPAT on motor motivational
performance. WAY 100635 blocks the inhibitory action of
8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at
doses which has no inhibitory action per se.

In behavioural models, WAY
100635 itself induces no overt behavioural changes but potently
antagonises the behavioural syndrome induced by 8-OH-DPAT in the rat and
guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01
mg/kg s.c., respectively). WAY 100635 also blocks the hypothermia
induced by 8-OH-DPAT in the mouse and rat with ID50 values of 0.01 mg/kg
s.c.

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Product Categories : Neuronal Signaling > 5-HT Receptor Inhibitor