WAY-100135

Names

[ Name ]:
WAY-100135

[Synonym ]:
3-[4-(2-Methoxyphenyl)piperazin-1-yl]-2-phenyl-N-tert-butyl-propanamide dihydrochloride
N-tert-butyl-3-[4-(2-methoxyphenyl)piperazin-1-yl]-2-phenylpropanamide,dihydrochloride
WAY-100135 dihydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1A Receptor:34 nM (IC50)

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₃₅Cl₂N₃O₂

[ Molecular Weight ]:
468.46000

[ Exact Mass ]:
467.21100

[ PSA ]:
48.30000

[ LogP ]:
5.96290

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport