| Description | WAY-100135 dihydrochloride is a potent and selective antagonist of both presynaptic and postsynaptic 5-HT 1A receptors, exhibiting an IC 50 value of 34 nM specifically at the rat hippocampal 5-HT 1A receptor. This compound displays promising antipsychotic effects. |
| In vitro | WAY100135 (0.1-1 μM) antagonises electrically evoked contractions of 5-carboxamidoiodotryptamine in the guinea-pig ileum, with a pA 2 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]. |
| Target activity | 5-HT1A receptor:34 nM (IC50) |
| molecular weight | 468.46 |
| Molecular formula | C24H35Cl2N3O2 |
| CAS | 149055-79-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 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. |