Ketamine salts solubility

[sekio]

I think mushrooms will 4-hydroxylate many simple N-alkylated tryptamines. Not sure about 5-MeO-xxx... due to the 5-methoxy being "fairly close" to 4- position I could even see 5-MeO-xxx being inhibitory on tryptamine 4-hydroxylation. (maybe 4-F-dmt is?)

They definitely won't hydroxylate people that's fo sho.

 

[sekio]

J Ethnopharmacol. 2010 Mar 2;128(1):160-5. Epub 2010 Jan 11.
The memory-enhancing effects of Euphoria longan fruit extract in mice.

AIM OF THE STUDY:

The fruit of Euphoria longan (Lour.) Steud. (Sapindaceae) is sweet and edible. Dried Euphoria longan fruit is prescribed as a tonic and for the treatment of forgetfulness, insomnia, or palpitations caused by fright in traditional Chinese medicine. The effects of aqueous extract of Euphoria longan fruit (ELE) on learning and memory and their underlying mechanisms were investigated.
MATERIALS AND METHODS:

Aqueous extract of Euphoria longan fruit (ELE) was administered to ICR mice for 14 days. Piracetam was used as a positive control for its known memory-enhancing effects. Memory performances were assessed using the passive avoidance task. The expressions of phosphorylated extracellular signal-regulated kinase (pERK) 1/2, phosphorylated cAMP response element binding protein (pCREB), brain-derived neurotrophic factor (BDNF), doublecortin (DCX) and the incorporation of 5-bromo-2-deoxyuridine (BrdU) in hippocampal dentate gyrus and CA1 regions were investigated using immunohistochemical methods.
RESULTS:

The step-through latency in the ELE-treated group was significantly increased compared with that in the vehicle-treated controls (P<0.05) in the passive avoidance task. Piracetam-treated group also showed enhanced cognitive performaces in the passive avoidance task. Immunohistochemical studies revealed that the number of cells immunopositive for BDNF, pCREB, or pERK 1/2 was significantly increased in the hippocampal dentate gyrus and CA1 regions after ELE treatment for 14 days (P<0.05). DCX and BrdU immunostaining also revealed that ELE significantly enhanced immature neuronal survival, but not neuronal cell proliferation in the subgranular zone of the dentate gyrus.
CONCLUSIONS:

The present results suggest that subchronic administration of aqueous extract of Euphoria longan fruit enhances learning and memory, and that its beneficial effects are mediated, in part, by BDNF expression and immature neuronal survival.

 

[Cortexiphan]

trans-2-(2,5-Dimethoxy-4-iodophenyl)cyclopropylamine and trans-2-(2,5-dimethoxy-4-bromophenyl)cyclopropylamine as potent agonists for the 5-HT₂ receptor family

Cyclopropyl analogues of DOB and DOI by Nichols et al.

Abstract

A strategy to replace the ethylamine side chain of 2,5-dimethoxy-4-iodoamphetamine (DOI, 1a), and 2,5-dimethoxy-4-bromoamphetamine (DOB, 1b) with a cyclopropylamine moiety was successful in leading to compounds with high affinity at the 5-HT₂ family of receptors; and the more potent stereoisomer of the cyclopropane analogues had the expected (−)-(1R,2S)-configuration. Screening for affinity at various serotonin receptor subtypes, however, revealed that the cyclopropane congeners also had increased affinity at several sites in addition to the 5-HT2A and 5-HT2B receptors. Therefore, at appropriate doses – although (−)-4 and (−)-5 may be useful as tools to probe 5-HT₂ receptor function – one would need to be mindful that their selectivity for 5-HT_2A receptors is somewhat less than for DOI itself.

Keywords: cyclopropanation; diazomethane; hallucinogen; 5-HT_2A agonist; receptor probe; trans-2-phenylcyclopropylamines

 

[pharmakos]

sekio, your new THUG LIFE avatar startled me at first when i saw it out of the corner of my eye. then it made me laugh very hard the second time it flashed and i actually read it.

at least i think its new.

 

[Thou]

I've been considering hydroxylating my mother.

For her own good, of course.

If this turns into legal discussion it will get locked forever, too, I gather.

 

[Jktm]

To turn into legal discussion, that would imply that there was conversation going on in here.

 

[ebola?]

I've been considering hydroxylating my mother.

If you liked it, you should have put a methylene-dioxy ring on it.

ebola

 

[Thou]

^She doesn't deserve it.

 

[pharmakos]

 

[Thou]

lol dude

 

[doppelgänger1]

DPP IV inhibitor blocks mescaline-induced scratching and amphetamine-induced hyperactivity in mice.

Abstract
Dipeptidyl peptidase IV (DPP IV) is a ubiquitous membrane-bound enzyme that cleaves the two N-terminal amino acids from peptides with a proline or alanine residue in the second position from the amino end. Potential substrates for DPP IV include several neuropeptides, suggesting a role for DPP IV in neurological processes. We have developed a potent DPP IV inhibitor (IC50 = 30 nM), 1-(2-amino-3-methyl-butyryl)-azetidine-2-carbonitrile (AMAC), which has shown efficacy in two established models of psychosis: mescaline-induced scratching and amphetamine-induced hyperactivity. In the mescaline-induced scratching model, AMAC treatment before mescaline administration reduced the number of scratching paroxysms by 68% (P < 0.01). The compound showed a dose-dependent effect, inhibiting significantly at 6, 20 and 60 mg/kg (37%, 39% and 68%, respectively). In the amphetamine-induced hyperactivity model, 50 and 60 mg/kg AMAC, given before injection of amphetamine, significantly reduced hyper-locomotion by 65% and 76%, respectively. Additionally, AMAC showed no significant activity in binding assays for 20 receptors thought to be involved in the pathology of schizophrenia, including dopamine, serotonin and glutamate. A structurally similar analog, 1-(2-dimethylamino-3-methyl-butyryl)-azetidine-2-carbonitrile (DAMAC), that does not inhibit DPP IV, was inactive in both models. Taken together, these data suggest that the antipsychotic effects of AMAC are the result of DPP IV inhibition.

Naloxone potentiates the disruptive effects of mescaline on operant responding in the rat.

Abstract
Food-deprived male rats were trained to press a lever on a fixed ratio-40 (FR-40) operant schedule for food reinforcement. Administration of mescaline (4.0--10.0 mg/kg) immediately before the start of the operant session resulted in a cessation of responding for some portion of the 40-min period ("hallucinatory pause"). The duration of this pause was found to be dose-dependent. Although administration of naloxone alone (1.0-8.0 mg/kg, five minutes prior to the start of the session) had no effect on FR-40 responding per se, pretreatment with this agent significantly potentiated the disruptive effects of mescaline. This potentiation by naloxone was further shown to be dose-dependent. These data suggest that the effects of the phenethylamine hallucinogen mescaline are potentiated by pretreatment with the narcotic antagonist naloxone.

 

[Captain.Heroin]

No posts for 10 days? What are you all busy doing?

 

[pharmakos]

No posts for 10 days? What are you all busy doing?

no synthesis discussion =p

lol j/k

 

[Thou]

I'm trying to get to the moon using two magnets and will power.

 

[sekio]

dont be a pussy. use chlorine trifluroride and hydrazine.

 

[Thou]

Oh the error of my ways.


Godamnit sekio.

If you're in the states I'll pay you 50 an hour to teach me kitchen chemistry. My luck your'e in Australia.

All the best ones are...


A neutron walks into a bar and orders 10 shots of whiskey. After he's had enough, he asks for his tab. The bartender says, "for you, no charge."


yar yar yar yar!

 

[sekio]

Confirmation that there is a genetically linked component to cannabis psychosis susceptibility

In a case-control study of 489 first-episode psychosis patients and 278 control subjects, we investigated the interaction between variation at the AKT1 rs2494732 single nucleotide polymorphism and cannabis use in increasing the risk of psychosis. [...] Carriers of the C/C genotype with a history of cannabis use showed a greater than twofold increased likelihood of a psychotic disorder (odds ratio = 2.18 [95% confidence interval: 1.12, 4.31]) when compared with users who were T/T carriers.

http://www.biologicalpsychiatryjournal.com/article/S0006-3223(12)00555-0/abstract

just goes to show how deep biochemistry is.

 

[Captain.Heroin]

If you're in the states I'll pay you 50 an hour to teach me kitchen chemistry.

He makes more than four times that stripping... but maybe he'll consider teaching you kitchen chemistry 1/4th the effort.

I kid, I kid...

I also had a lol about your neutron in a bar joke.

 

[pharmakos]

my chemistry teacher in college said he once had a student that was in Kappa Iota. student came into class wearing a sweater with his fraternity letters on it, so teacher made the student take a picture while holding a model of Potassium Iodide.

 

[Transform]

http://www.sciencedirect.com/science/article/pii/S0014299912010114

Fourteen substances from the class of drugs sometimes known as “legal highs” were screened against a battery of human receptors in binding assays, and their potencies as inhibitors of monoamine uptake determined in functional in vitro assays.

Thirteen of the test substances acted as inhibitors of monoamine uptake at submicromolar concentrations, including 9 potent inhibitors of the dopamine transporter (DAT), 12 potent inhibitors of the norepinephrine transporter (NET) and 4 potent inhibitors of the serotonin transporter (SERT). Seven compounds acted as submicromolar inhibitors of both DAT and NET, and three substances 1-(benzofuran-5-yl)propan-2-amine (5-APB), 1-naphthalen-2-yl-2-pyrrolidin-1-ylpentan-1-one hydrochloride (“naphyrone”) and 1-naphthalen-1-yl-2-pyrrolidin-1-ylpentan-1-one hydrochloride (“1-naphyrone”) were submicromolar inhibitors of all three monoamine transporters.

There was a lack of correlation between results of functional uptake experiments and in vitro binding assays for the monoamine transporters. There was also no correlation between the human behavioral effects of the substances and the results of bindings assays for a range of receptor targets, although 1-(benzofuran-5-yl)propan-2-amine (5-APB), 1-(benzofuran-6-yl)propan-2-amine hydrochloride (6-APB) and 5-iodo-2,3-dihydro-1H-inden-2-amine hydrochloride (5-iodo-aminoindane) exhibited <100 nM affinities for 5HT2B and α2C receptors. Functional assays revealed that 5-APB and 6-APB were potent full agonists at 5HT2B receptors.