Top 10 similar words or synonyms for eptapirone

sarizotan    0.919838

sunepitron    0.908599

milipertine    0.897684

binospirone    0.897659

befiradol    0.894268

ciclazindol    0.893658

tandamine    0.893438

faverin    0.892986

mosapramine    0.892318

repinotan    0.891237

Top 30 analogous words or synonyms for eptapirone

Article Example
Eptapirone In the conflict procedure, eptapirone produced substantial increases in punished responding without affecting unpunished responding, which was suggestive of marked anxiolytic-like effects. In addition, the efficacy of eptapirone in this assay was more evident than that of buspirone, ipsapirone, and flesinoxan.
Eptapirone In the Porsolt forced swimming test, eptapirone was found to suppress immobility more robustly than buspirone, ipsapirone, flesinoxan, paroxetine, and imipramine, which was suggestive of strong antidepressant-like effects. In this assay, unlike the other drugs screened, buspirone actually "increased" the immobility time with a single administration, while repeated administration decreased it, an effect that may have been related to buspirone's relatively weak intrinsic activity (~30%) at the 5-HT receptor and/or its preferential activation of 5-HT somatodendritic autoreceptors over postsynaptic receptors.
Eptapirone Eptapirone has been assayed in humans in preclinical trials at an oral dose of 1.5 mg. In these studies, eptapirone reduced body temperature, prolonged REM sleep, increased cortisol and growth hormone levels, and produced side effects such as dizziness and drowsiness while being overall well-tolerated. It peaked rapidly within 30–60 minutes and had an estimated half-life of two hours, with a total duration of approximately three hours.
Eptapirone Eptapirone (F-11,440) is a very potent and highly selective 5-HT receptor full agonist of the azapirone family. Its affinity for the 5-HT receptor was reported to be 4.8 nM (K) (or 8.33 (pK)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%).
Eptapirone Eptapirone and related high-efficacy 5-HT full and super agonists such as befiradol and F-15,599 were developed under the hypothesis that the maximum exploitable therapeutic benefits of 5-HT receptor agonists might not be able to be seen without the drugs employed possessing sufficiently high intrinsic activity at the receptor. As 5-HT receptor agonism, based on animal and other research, looked extremely promising for the treatment of depression from a theoretical perspective, this idea was developed as a potential explanation for the relatively modest clinical effectiveness seen with already available 5-HT receptor agonists like buspirone and tandospirone, which act merely as weak-to-moderate partial agonists of the receptor.
Eptapirone After repeated administration, high dose paroxetine was able to rival the reduction in immobility seen with eptapirone. However, efficacy was seen on the first treatment with eptapirone, which suggested that eptapirone may have the potential for a more rapid onset of antidepressant effectiveness in comparison. Imipramine was unable to match the efficacy of eptapirone or high dose paroxetine, which was probably the result of the fact that higher doses were fatal.
Azapirone 5-HT receptor partial agonists have demonstrated efficacy against depression in rodent studies and human clinical trials. Unfortunately, however, their efficacy is limited and they are only relatively mild antidepressants. Instead of being used as monotherapy treatments, they are more commonly employed as augmentations to serotonergic antidepressants like the SSRIs. It has been proposed that high intrinsic activity at 5-HT postsynaptic receptors is necessary for maximal therapeutic benefits to come to prominence, and as a result, investigation has commenced in azapirones which act as 5-HT receptor full agonists such as alnespirone and eptapirone. Indeed, in preclinical studies, eptapirone produces robust antidepressant effects which surpass those of even high doses of imipramine and paroxetine.