Kingpinguin
Member
- Joined
- Aug 14, 2019
- Messages
- 586
Hi!
So according to many sources cyphroheptadine is a quite potent D3 antagonist.
D3 agonists show antidepressant effects and also strong increase in reward seeking behaviour, sexual desire and libido. I’ve personally noticed reduced desire, libido, motivation on higher doses of cyphroheptadine. But I’ve been looking for an good easy serotonin antagonist which mainly acts on the 5-ht2 receptors since most bad effects of serotonin are om these receptors. But with as little 5-ht1a antagonism and dopamine antagonism. 5-ht1a and 5-ht2c seems to be each others polar opposites where as one reduces dopamine, motivation sexual desire and the other reduces motivation, lowers dopamine, increases cortisol and prolactin. But finding a substance that seems safe/well researched does seem rather hard.
Metergoline seems to be one of the best options but it still antagonist at 5-ht1a.
anyway the antagonism of 5-ht1a of cyphroheptadine seems to be 59 nanomol (i assume this antagonism happens at 59 nanomol per liter? If anyone knows how to explain I’d appreciate that).
But all the 5-ht2 receptors only require 1-2 nM.
and D3 receptor 8 nM
So from the internet I found:
In 1L —-> 100 000ng/11000nmol =
9.09 nM
So my assumption a dose of 0,5mg fully absorbed cyphroheptadine would amount to 500 000ng in 1L. Humans contain about 4,7-5,5 liters of blood so lets say 5 liters then.
So now you can divide the 500 000ng back to 100 000ng again.
So this would mean with a cyphro dose of 0,5 you would hit 9,09 nM levels in your blood and that will be enough to have affinity for the dopamine D3 receptor as an antagonist which is at 8 nM.
Anyone who can answer if my thought pattern is correct?
Now I know absorption is not 100% and theres other variables to calculate for but you can at least halve the recommended dose of 0,5mg to get 0,25mg and a blood concentration of 4,5 nM which still would give a antagonistic effect of the bad 5-ht2 receptors with negliable effect on the dopamine system.
appreciate help with this calculation if anyone possess more knowledge than me how to calculate it precisly or if I’ve made any errors.
Need to find the oral dose of cyphroheptadine to obtain an nM level of 2,5-7 nM
@Cirion
I know you have a brain of a statistician. Think this calculation could be a interesting micro project for you
Peace
Homies.
So according to many sources cyphroheptadine is a quite potent D3 antagonist.
D3 agonists show antidepressant effects and also strong increase in reward seeking behaviour, sexual desire and libido. I’ve personally noticed reduced desire, libido, motivation on higher doses of cyphroheptadine. But I’ve been looking for an good easy serotonin antagonist which mainly acts on the 5-ht2 receptors since most bad effects of serotonin are om these receptors. But with as little 5-ht1a antagonism and dopamine antagonism. 5-ht1a and 5-ht2c seems to be each others polar opposites where as one reduces dopamine, motivation sexual desire and the other reduces motivation, lowers dopamine, increases cortisol and prolactin. But finding a substance that seems safe/well researched does seem rather hard.
Metergoline seems to be one of the best options but it still antagonist at 5-ht1a.
anyway the antagonism of 5-ht1a of cyphroheptadine seems to be 59 nanomol (i assume this antagonism happens at 59 nanomol per liter? If anyone knows how to explain I’d appreciate that).
But all the 5-ht2 receptors only require 1-2 nM.
and D3 receptor 8 nM
So from the internet I found:
In 1L —-> 100 000ng/11000nmol =
9.09 nM
So my assumption a dose of 0,5mg fully absorbed cyphroheptadine would amount to 500 000ng in 1L. Humans contain about 4,7-5,5 liters of blood so lets say 5 liters then.
So now you can divide the 500 000ng back to 100 000ng again.
So this would mean with a cyphro dose of 0,5 you would hit 9,09 nM levels in your blood and that will be enough to have affinity for the dopamine D3 receptor as an antagonist which is at 8 nM.
Anyone who can answer if my thought pattern is correct?
Now I know absorption is not 100% and theres other variables to calculate for but you can at least halve the recommended dose of 0,5mg to get 0,25mg and a blood concentration of 4,5 nM which still would give a antagonistic effect of the bad 5-ht2 receptors with negliable effect on the dopamine system.
appreciate help with this calculation if anyone possess more knowledge than me how to calculate it precisly or if I’ve made any errors.
Need to find the oral dose of cyphroheptadine to obtain an nM level of 2,5-7 nM
@Cirion
I know you have a brain of a statistician. Think this calculation could be a interesting micro project for you
Peace
Homies.
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