Area-1255

Area-1255's official forum for all of our life extension enthusiasts, bodybuilders, fitness geeks and for those just interested in science and technology.


You are not connected. Please login or register

How to sleep well but see dreams. Not wet yet

View previous topic View next topic Go down  Message [Page 1 of 1]

1 How to sleep well but see dreams. Not wet yet on Sun Aug 21, 2016 4:10 am

kpavel

avatar
Area-1255 Intelligence Oversight
Area-1255 Intelligence Oversight
Last autumn I noticed that I didn't wake up through the night since summer. What could be this. This is Seditol by Source Naturals I think. And here's the scientific note:
Moriarty SR1, Hedley L, Flores J, Martin R, Kilduff TS. wrote:Selective 5HT2A and 5HT6 receptor antagonists promote sleep in rats.
STUDY OBJECTIVES:
Serotonin (5-HT) has long been implicated in the control of sleep and wakefulness. This study evaluated the hypnotic efficacy of the 5-HT6 antagonist RO4368554 (RO) and the 5-HT2A receptor antagonist MDL100907 (MDL) relative to zolpidem.
DESIGN:
A randomized, repeated-measures design was utilized in which Wistar rats received intraperitoneal injections of RO (1.0, 3.0, and 10 mg/kg), MDL (0.1, 1.0 and 3.0 mg/kg), zolpidem (10 mg/kg), or vehicle in the middle of the dark (active) period. Electroencephalogram, electromyogram, body temperature (Tb) and locomotor activity were analyzed for 6 hours after injection.
MEASUREMENTS AND RESULTS:
RO, MDL, and zolpidem all produced significant increases in sleep and decreases in waking, compared with vehicle control. All 3 doses of MDL produced more consolidated sleep, increased non-rapid eye movement sleep (NREM) sleep, and increased electroencephalographic delta power during NREM sleep. The highest dose of RO (10.0 mg/kg) produced significant increases in sleep and decreases in waking during hour 2 following dosing. These increases in sleep duration were associated with greater delta power during NREM sleep. ZO Zolpidem induced sleep with the shortest latency and significantly increased NREM sleep and delta power but also suppressed rapid eye movement sleep sleep; in contrast, neither RO nor MDL affected rapid eye movement sleep. Whereas RO did not affect Tb, both zolpidem and MDL reduced Tb relative to vehicle-injected controls.
CONCLUSIONS:
These results support a role for 5-HT2A receptor modulation in NREM sleep and suggest a previously unrecognized role for 5-HT6 receptors in sleep-wake regulation.
There is actually another korean alternative for this receptor:
KIM DH1, KIM SH, KIM HJ, Jin C, Chung KC, Rhim H. wrote:Stilbene derivatives as human 5-HT(6) receptor antagonists from the root of Caragana sinica.
The 5-HT₆ receptor (5-HT₆R) is a member of the class of recently discovered 5-hydroxytryptamine (5-HT) receptors. Due to the lack of selective 5-HT₆R ligands, the cellular signaling mechanisms of the 5-HT₆R are poorly understood. We previously developed a cell-based high-throughput screening (HTS) method for the 5-HT₆R and screened synthetic chemical compounds. In the present study, we expanded our screening into natural products to find novel 5-HT₆R ligands. We found that the ethyl acetate fraction from the root of Caragana sinica (537-18BE) produced the most potent antagonistic activity. After further isolation of 537-18BE, we found that three stilbene derivatives, (+)-α-viniferin, miyabenol C and pallidol, are active constituents of 537-18BE inhibiting the 5-HT₆R. Among them, (+)-α-viniferin showed the most potent inhibition, and miyabenol C also produced a considerable inhibition. When examined effects on other neurotransmitters for selectivity, 537-18BE and three stilbene derivatives did not produce any notable effects on 5-HT₄, 5-HT₇, or muscarinic acetylcholine M1 (M(1)) receptors. Furthermore, 5-HT₆R antagonistic effects of (+)-α-viniferin, miyabenol C and pallidol were confirmed on extracellular signal-regulated kinase 1 and 2 (ERK1/2) which exerts effects in downstream pathways of 5-HT₆R activation.
Now you can sleep well comrades Cool

Area-1255

avatar
Admin / Head Writer
Admin / Head Writer
Yeup, that does make sense. 5-HT2A-antagonism in humans tends to lower blood pressure, Cortisol, ACTH and promote sleep; as indicated with Risperidone & Ritanserin being well known serotonin antagonists. These have a sedative property, however, their antihistamine effects are more potent and cause the majority of sedation despite their anti-serotonin properties. Serotonin blockade via 5-HT1A receptors would help balance out the 2A antagonist effects in terms of alertness, mood etc but either way, anti-serotonin agents are beneficial for hormone homeostasis IF other properties (i.e anti-dopamine) are not also being implemented.

Therefore agents like Ketanserin or Ritanserin have benefits while Risperdal has negative effects despite its anti-serotonin properties, the anti-dopamine effects negate the benefits (mostly) of its anti-serotonin action.

The 5-HT6 action is interesting, although not entirely surprising, as Magnolia Officinalis extract is a 5-HT6 antagonist and has sedative/anti-anxiety properties. Though, I think in humans, antagonism at that receptor would be less relevant for sleep and more relevant to memory.

Arrow http://www.ncbi.nlm.nih.gov/pubmed/19505549
Arrow http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3706851/
Arrow http://www.nature.com/npp/journal/v21/n3/full/1395376a.html

http://area-1255.forumotion.info

View previous topic View next topic Back to top  Message [Page 1 of 1]

Permissions in this forum:
You cannot reply to topics in this forum