Disease relevance of Way 100135

• Both pindolol, a nonselective 5-HT1A receptor/beta adrenoceptor antagonist and n-t-butyl,-3-[1-[4-(2-methoxy)phenyl]piperazinyl]-1-phenylpropionamid e [(+) WAY 100135], a more selective 5-HT1A receptor antagonist, dose dependently attenuated the hypothermia induced by all three agonists [1].

Psychiatry related information on Way 100135

• Given alone, WAY 100135 had no effect on the locomotor activity of rats; 2) WAY 100135 (1.25 and 2.5 mg/kg, but not 10 or 20 mg/kg), attenuated or abolished the disruptive effects of MK-801 on the sensorimotor gating measured in a prepulse-induced inhibition of the acoustic startle response paradigm [2].

High impact information on Way 100135

• This inhibition was not affected by previous systemic application of either the selective 5HT1A receptor antagonist (+)WAY 100135 or by the 5HT2 receptor antagonist mesulergine, whereas pretreatment with the nonselective 5HT1 antagonist methiothepin significantly attenuated the effect of TFMPP [3].
• The effect of 8-OH-DPAT was reversed by WAY 100135 [N-tert-butyl-3-[1-[1-(2-methoxy)phenyl]piperazinyl]-1-phenylpropiona mide; a 5-HT1A antagonist] [4].
• The 5-HT(1A) receptor agonist buspirone relaxed fundic smooth muscle, and the relaxation was inhibited by WAY-100135 but not by N(omega)-nitro-l-arginine or tetrodotoxin [5].
• These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN [6].
• The decrease in heart rate produced by i.v. bolus doses of flesinoxan or U-93385 was reversed by administration of the 5-HT1A receptor antagonists spiperone or WAY 100135 [7].

Biological context of Way 100135

• WAY-100135 on its own did not affect food intake [8].
• Structure-activity relationship studies of CNS agents. Part 24: New analogs of N-tert.-butyl-3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenylpropanamide (WAY-100135) [9].

Anatomical context of Way 100135

• Again, given alone, WAY 100135 did not influence the behavior of rats in that experimental paradigm; and 4) MK-801 (0.4 mg/kg) had no effect on the 5-HT1A receptor mRNA level in rat hippocampus, measured 2 and 24 hours after MK-801 administration [2].
• The antagonist actions of WAY-100135 and its enantiomers on 5-HT1A receptor-mediated hyperpolarization of the rat isolated superior cervical ganglion [10].
• The present study investigated the effects of these drugs, as well as the 5-HT1A receptor antagonist WAY 100135 (N-tert-butyl-3-(4-(2-methoxyphenyl)piperazine-1-yl)-2-phenylpropanamide ) injected into the midbrain periaqueductal gray matter of mice on 30-bites analgesia [11].

Associations of Way 100135 with other chemical compounds

• The effects of a low dose of 5-HT (3.2 microM) on fPS, Vr and R in were reversed by the specific 5-HT(1A)-receptor antagonist WAY 100135 (10 microM). cOA (1 microM) failed to potentiate 5-HT1A receptor mediated effects on fPS, Vr or R in [12].
• Antidepressant properties of 5-HT1A receptor ligands (the full agonist 8-OH-DPAT, the partial agonists ipsapirone and buspirone, and the selective antagonist WAY 100135) were studied in a chronic mild stress model of depression [13].
• As 5-hydroxytryptamine1A (5-HT1A) receptors are enriched on cell bodies of corticostriatal neurones, a selective 5-HT1A-antagonist (WAY 100135) was coapplied with the lower dose of NMDA [14].
• The full 5-HT1A receptor agonist BAY R 1531 blocked, whereas, WAY 100135 and gepirone intensified 30-bites analgesia [11].
• In order to assess whether these ligands decrease 5-HT release by stimulating 5-HT1A receptors we examined the ability of the selective 5-HT1A receptor antagonist N-tert-butyl 3-4-(2-methoxyphenyl) piperazin-1-yl-2-phenylpropanamide dihydrochloride (WAY-100135) to block their inhibitory effects on 5-HT [15].

Gene context of Way 100135

• The effect of the two last drugs was antagonized by WAY-100135, a selective 5-HT1A receptor antagonist [16].
• Furthermore, the 5-HT1A receptor antagonist WAY 100135 did not protect DBA/2J mice from audiogenic seizures at doses that antagonise 5-HT1A receptor-mediated effects in mice [17].

Analytical, diagnostic and therapeutic context of Way 100135

• This effect was antagonized by a previous microinjection of (+)WAY-100135 (40 nmol/0.5 microliter), a selective 5-HT1A antagonist [18].

References