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WAY-100135 dihydrochloride

CAS: 149055-79-8 F: C24H35Cl2N3O2 W: 468.46

WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34
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Bioactivity WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties[1][2].
Invitro WAY100135 (0.1-1 μM) antagonises electrically evoked contractions of 5-carboxamidoiodotryptamine in the guinea-pig ileum, with a pA2 of 7.2[1].WAY-100135 dihydrochloride (10 μM) blocks the suppressive effect of 8-OH-DPAT on eEPSC and eIPSC in MVM neurons[2].
In Vivo WAY100135 (2.5 mg/kg) induces a maximum 30% inhibition of raphe neuronal firing and (0.5 mg/kg i.v.) antagonises the inhibition of firing induced by 8-OH-DPAT in anaesthetised rats[1].WAY-100135 dihydrochloride (10 mM; 1 μL for microinjection) effectively abolishes all 5-HT induced behavioural deficits in rats[2].
Name WAY-100135 dihydrochloride
CAS 149055-79-8
Formula C24H35Cl2N3O2
Molar Mass 468.46
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [1]. Fletcher A, et, al. WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. Eur J Pharmacol. 1993 Jun 24;237(2-3):283-91. [2]. Han L, et, al. 5-HT 1A receptor-mediated attenuation of synaptic transmission in rat medial vestibular nucleus impacts on vestibular-related motor function. J Physiol. 2021 Jan;599(1):253-267.