WAY 100135 dihydrochloride - CAS 149055-79-8
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor
WAY 100135 dihydrochloride is a selective 5-HT1A antagonist (IC50 = 15 nM).
Brife Description:
5-HT1A antagonist
White Solid
WAY 100135 hydrochloride; WAY100135 hydrochloride; WAY-100135 hydrochloride; 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
Melting Point:
>183°C (dec.)
Canonical SMILES:
1.Pain Inhibits Pain: an Ascending-Descending Pain Modulation Pathway Linking Mesolimbic and Classical Descending Mechanisms.
Tobaldini G;Sardi NF;Guilhen VA;Fischer L Mol Neurobiol. 2018 Jun 1. doi: 10.1007/s12035-018-1116-7. [Epub ahead of print]
The ability to modulate pain perception is as critical to survival as pain itself. The most known pain modulation pathway is the PAG-RVM (periaqueductal gray-rostral ventromedial medulla) descending system. In this study, we hypothesized that it is functionally linked to the ascending nociceptive control, which is a form of pain-induced analgesia dependent on mesolimbic mechanisms. To test this hypothesis, we used a pharmacological approach, in which the antinociception induced by noxious stimulation (forepaw injection of capsaicin) was detected in a standard rat model of inflammatory pain (hindpaw injection of carrageenan). This antinociception was blocked by interventions known to block the ascending nociceptive control-mediated analgesia: the blockade of μ-opioid (Cys;2;,Tyr;3;,Orn;5;,Pen;7;amide (CTOP) 0.5 μg) or of dopamine (SCH23390 1.8 μg and raclopride 5 μg) receptors within the NAc (nucleus accumbens) and that of cholinergic nicotinic receptors (mecamylamine 0.6 μg) within the RVM. The antinociception was also blocked by standard interventions known to block mechanisms of descending inhibition within either the PAG or the RVM: local acute neuronal blockade (lidocaine 2%), blockade of μ-opioid receptors (CTOP 0.
2.Serotonin antagonists do not attenuate activity-induced phase shifts of circadian rhythms in the Syrian hamster.
Antle MC;Marchant EG;Niel L;Mistlberger RE Brain Res. 1998 Nov 30;813(1):139-49.
A variety of observations from several rodent species suggest that a serotonin (5-HT) input to the suprachiasmatic nucleus (SCN) circadian pacemaker may play a role in resetting or entrainment of circadian rhythms by non-photic stimuli such as scheduled wheel running. If 5-HT activity within the SCN is necessary for activity-induced phase shifting, then it should be possible to block or attenuate these phase shifts by reducing 5-HT release or by blocking post-synaptic 5-HT receptors. Animals received one of four serotonergic drugs and were then locked in a novel wheel for 3 h during the mid-rest phase, when novelty-induced activity produces maximal phase advance shifts. Drugs tested at several doses were metergoline (5-HT1/2 antagonist; i.p.), (+)-WAY100135 (5-HT1A postsynaptic antagonist, which may also reduce 5-HT release by an agonist effect at 5-HT1A raphe autoreceptors; i.p.), NAN-190 (5-HT1A postsynaptic antagonist, which also reduces 5-HT release via an agonist effect at 5-HT1A raphe autoreceptors; i.p.) and ritanserin (5-HT2/7 antagonist; i.p. and i.c.v.). Mean and maximal phase shifts to running in novel wheels were not significantly affected by any drug at any dose. These results do not support a hypothesis that 5-HT release or activity at 5HT1, 2 and 7 receptors in the SCN is necessary for the production of activity-induced phase shifts in hamsters.
3.The novel buspirone analogue, 8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)[butyl]-8-azaspiro [4.5 ]decane-7,9-dione, with anxiolytic-like and antidepressant-like effects in rats.
Dereń-Wesołek A;Tatarczyńska E;Chojnacka-Wójcik E J Psychopharmacol. 1998;12(4):380-4.
In the conflict drinking test, used as a model to examine anxiolytic-like activity, the novel buspirone analogue 8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)]butyl)-8-azaspiro[ 4.5]decane-7,9-dione (MM199) (0.62-2.5 mg/kg) and buspirone (0.62-5 mg/kg), significantly increased the punished drinking in water-deprived rats, without affecting water consumption or perception of the stimulus. The anticonflict activity of MM199 (1.25 mg/kg) was blocked by (S)-WAY 100135 (20 mg/kg), a 5-hydroxytrypatmine1A (5-HT1A) receptor antagonist. In the forced swimming test, used as a model to examine the antidepressant-like activity, MM199 (5-20 mg/kg) reduced the immobility time, while buspirone (5-20 mg/kg) had no such effect. The reduced immobility induced by MM199 (20 mg/kg) was antagonized by (S)-WAY100135 (10 mg/kg). The above findings suggest that MM199 possesses potent anxiolytic- and antidepressant-like properties which are mediated by activation of 5-HT1A receptors.
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CAS 149055-79-8 WAY 100135 dihydrochloride

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