3 Matching Annotations
  1. Jan 2021
    1. IC50 values for histamine-H1, dopamine-D2, and adrenergic-alpha 1 and -alpha 2 sites were 39-, 77-, 107-, and 166-fold higher

      Thus, ritanserin is highly selective for 5HT2 receptors. By comparison, ketanserin antagonizes.adrenergic alpha 1 in addition to serotonin receptors.

  2. Dec 2020
    1. The 5-HT2 antagonists reportedly produce a paradoxical down-regulation of 5-HT2 binding sites upon chronic treatment, rather than the expected supersensitivity. Chronic treatment with ritanserin (2.5 mg/kg/day for 7 days), but not mianserin (same regimen), attenuated a QMWS 24 h after the final injection, thus supporting with a functional measure, the down-regulation of such binding sites by ritanserin.

      Are they saying that mianserin did not downregulate the receptors? That's what it sounds like. Most likely this is just because it is a weaker antagonist than ritanserin.

    1. In contrast, ritanserin did not impair driving performance or affect objectively measured daytime sleepiness, while subjects reported to feel more alert during daytime.

      Fascinating. This increased subjective alertness is probably due to enhanced sleep.