Comment · Wed, August 14, 2013
Mdma and pooping
Original post in this thread
[deleted] · 19 points
DAE poop more than usual the next few days? Why is that?
What they were answering
reductase · 1 points
Hmm... have you looked into sarpogrelate? Based on what its used to treat, it seems peripherally active without crossing the BBB and having an antipsychotic effect typical of centrally active 5HT2 antagonists.
As I am no longer at work I don't have access to full-text articles to help you out much more than wiki links.
u/MisterYouAreSoDumb
Hmmm, that would be an interesting way to attack it. Inhibit 5-HT2B in the periphery, but not centrally.
Antinociception in rat by sarpogrelate, a selective 5-HT receptor 2A antagonist, is peripheral
> While these effects
might be derived from a supraspinal antinociceptive action
of the drug, sarpogrelate penetrates the blood–brain barrier
only minimally. According to information supplied by the
manufacturers, the brain tissue concentration of sarpogre-
late was 0.25–0.5% of the plasma concentration, in a
w
14
x tracer experiment using C -labeled sarpogrelate Mitsubishi Kasei, unpublished data . Therefore, antinociception
from intraperitoneal administration of the drug probably
involves a mainly peripheral action.
Effects of a 5-HT 2A receptor antagonist, sarpogrelate on thermal or inflammatory pain
>After oral administration of sarpogrelate to rats, the peak
sarpogrelate concentration in the brain and spinal cord was
about 2% of the plasma concentration (Komatsu et al.,
1991). Thus, sarpogrelate has very low permeability of the
blood–brain barrier. Therefore, intrathecally administered
sarpogrelate acts only in the brain or spinal cord, where 5-
HT 2 receptor agonists would be analgesic, and does not go
into systemic circulation and periphery.
It could be a good candidate!