Hive Tryptamine Chemistry

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	Tryptamine Chemistry

All 4 posts Subject: Cycloalkylamides of d-Lysergic Acid Please login to post Down

trade_om
(Stranger)
08-03-04 19:54
No 523438
      Cycloalkylamides of d-Lysergic Acid

Hello.
Ive been going through patents and found this one dating back from 1959. It describes how to synthesis cycloalkylamides of d-Lysergic Acid. It also states that cycloalkylamides of the acid have more anti-serotonin activity then lsd-25(5 fold).
Patent GB816273

Lilienthal
(Moderator)
08-15-04 12:28
No 525518
User Picture       That is interesting historically interesting.

That is interesting historically interesting. It was later found that hallucinogens act as serotonin-mimetics and not as anti-serotonergics at a certain subtype of serotonin receptors, i.e. they are agonists at the 5-HT2A receptor. smile

Nicodem
(Hive Bee)
08-15-04 17:51
No 525551
User Picture       Yes, but if they are partial agonists like...

Yes, but if they are partial agonists like LSD, they actually block the effect of serotonin in tissue preparations. They occupy the receptor sites but have a lower activity than serotonin itself. Hence LSD was said to have antiserotonin activity as it actually has but only relatively to serotonin. But now we are in the best years of neurochemistry and like Lily says, it’s historically interesting. smile

“The real drug-problem is that we need more and better drugs.” – J. Ott

7is
(Hive Bee)
08-18-04 01:19
No 525983
User Picture       Nichols

They don't have LSD-like effects according to Nichols:

Votava et al (1958) prepared a series of cycloalkyl monosubstituted amides in a series from aminocyclopropane
(a three-carbon ring system) through aminocycloheptane (a seven-carbon ring system). The aminocyclobutane and
aminocylopentane cycloalkylamides, shown above, gave antiserotonin effects in a rat intestine preparation that were
30% greater than LSD itself, but the compounds did not have LSD-like effects in man.

http://www.heffter.org/review/Review2/chap6.pdf

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	All 4 posts		Subject: Cycloalkylamides of d-Lysergic Acid		Please login to post		Down


		trade_om (Stranger) 08-03-04 19:54 No 523438				Cycloalkylamides of d-Lysergic Acid
						Hello. Ive been going through patents and found this one dating back from 1959. It describes how to synthesis cycloalkylamides of d-Lysergic Acid. It also states that cycloalkylamides of the acid have more anti-serotonin activity then lsd-25(5 fold). Patent GB816273



		Lilienthal (Moderator) 08-15-04 12:28 No 525518				That is interesting historically interesting.
						That is interesting historically interesting. It was later found that hallucinogens act as serotonin-mimetics and not as anti-serotonergics at a certain subtype of serotonin receptors, i.e. they are agonists at the 5-HT2A receptor.



		Nicodem (Hive Bee) 08-15-04 17:51 No 525551				Yes, but if they are partial agonists like...
						Yes, but if they are partial agonists like LSD, they actually block the effect of serotonin in tissue preparations. They occupy the receptor sites but have a lower activity than serotonin itself. Hence LSD was said to have antiserotonin activity as it actually has but only relatively to serotonin. But now we are in the best years of neurochemistry and like Lily says, it’s historically interesting. “The real drug-problem is that we need more and better drugs.” – J. Ott



		7is (Hive Bee) 08-18-04 01:19 No 525983				Nichols
						They don't have LSD-like effects according to Nichols: Votava et al (1958) prepared a series of cycloalkyl monosubstituted amides in a series from aminocyclopropane (a three-carbon ring system) through aminocycloheptane (a seven-carbon ring system). The aminocyclobutane and aminocylopentane cycloalkylamides, shown above, gave antiserotonin effects in a rat intestine preparation that were 30% greater than LSD itself, but the compounds did not have LSD-like effects in man. http://www.heffter.org/review/Review2/chap6.pdf

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