Tutkimusjulkaisut
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Tutkimusjulkaisut
Uploadaillaan tähän topiciin vertaisarvioiduissa tiedejulkaisuissa ilmestyneitä papereita kokonaisuudessaan. Nämä kallisarvoiset aineistot ovat usein maksuseinän takana ja asiasta kiinnostuneella ihmisellä ei välttämättä rahkeet riitä isojen summien pulittamiseen.
Informaation on tarkoitus olla vapaata!
Jos joitakin artikkeleja on hakusessa, niin niitä saa myös vapaasti pyydellä. Saattaa olla, että jonkun kovalevyltä löytyy.
HUOM: Liitetiedostot poistettu käytöstä ylläpidon toimesta 1. 3. 2014 lähtien.
En valitettavasti viitsi alkaa uploadailemaan noita mainittuja uusiksi mihinkään. LibGenistä ja Google Scholarista voi koittaa kalastella maksuseinän takana olevia julkaisuja.
Informaation on tarkoitus olla vapaata!
Jos joitakin artikkeleja on hakusessa, niin niitä saa myös vapaasti pyydellä. Saattaa olla, että jonkun kovalevyltä löytyy.
HUOM: Liitetiedostot poistettu käytöstä ylläpidon toimesta 1. 3. 2014 lähtien.
En valitettavasti viitsi alkaa uploadailemaan noita mainittuja uusiksi mihinkään. LibGenistä ja Google Scholarista voi koittaa kalastella maksuseinän takana olevia julkaisuja.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
Re: Koko paperi -dumppaustopic
Ei mulla oo mittää papereita dumpata, mutta haluun nyt kuitenki ilmaista kaiken arvostuksen ja hyväksyvän nyökyttelyni ketjun johdosta (plus BUMP!)
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Re: Koko paperi -dumppaustopic
Paria koitin vilkaista, mut tuntuu niin perhanan vaikeelta tekstiltä tutustua, että jätin kesken. Jokatapauksessa arvostan tällaista jakamista, ja ehkä joskus kykenen itsekin tajuamaan jotain mitä nää käsittelee. 

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Re: Koko paperi -dumppaustopic
MDPV:n psykofarmakologiaa ja MDPV:tä ilmiönä kastastava paperi tässä.
3,4-methylenedioxypyrovalerone (MDPV): chemistry, pharmacology and toxicology of a new designer drug of abuse marketed online. (Coppola M, Mondola R)
3,4-methylenedioxypyrovalerone (MDPV): chemistry, pharmacology and toxicology of a new designer drug of abuse marketed online. (Coppola M, Mondola R)
The illicit marketplace of substances of abuse continually offers for sale legal alternatives to controlled drugs to a large public. In recent years, a new group of designer drugs, the synthetic cathinones, has emerged as a new trend, particularly among young people. The 3,4-methylenedioxypyrovalerone (MDPV), one of this synthetic compounds, caused an international alert for its cardiovascular and neurological toxicity. This substance, sold as bath salts, has caused many serious intoxications and some deaths in several countries. The aim of this paper is summarise the clinical, pharmacological and toxicological information about this new designer drug.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Re: Koko paperi -dumppaustopic
Erowidin "What's New?" :sta napattu: Chemical Characterization of Methoxetamine
Kunpa auringon päivät päällämme ei päättyisi koskaan.
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Re: Koko paperi -dumppaustopic
Tuore stimulanttien metaboliaa kaaviokuvineen selvittävä kaksoismetoditutkimus tässä. Mun mielestäni kaikki markkinoille ujuttautuva laillinen douppi pitäis katsastaa tällä tavoin ennen kuin käyttö leviää käsiin ja meillä on uusi lauma dopaminergiset neuroninsa kärventäneitä ihmispökkelöitä.
Generation of metabolites by an automated online metabolism method using human liver microsomes with subsequent identification by LC-MS(n), and metabolism of 11 cathinones (Mueller DM, Rentsch KM. 2012)
Generation of metabolites by an automated online metabolism method using human liver microsomes with subsequent identification by LC-MS(n), and metabolism of 11 cathinones (Mueller DM, Rentsch KM. 2012)
Human liver microsomes (HLMs) are used to simulate human xenobiotic metabolism in vitro. In forensic and clinical toxicology, HLMs are popularly used to study the metabolism of new designer drugs for example. In this work, we present an automated online extraction system we developed for HLM experiments, which was compared to a classical offline approach. Furthermore, we present studies on the metabolism of 11 cathinones; for eight of these, the metabolism has not previously been reported. Metabolites were identified based on MS2 and MS3 scans. Fifty-three substances encompassing various classes of drugs were employed to compare the established offline and the new online methods. The metabolism of each of the following 11 cathinones was studied using the new method: 3,4-methylenedioxy-N-benzylcathinone, benzedrone, butylone, dimethylcathinone, ethylone, flephedrone, methedrone, methylone, methylethylcathinone, naphyrone, and pentylone. The agreement between the offline and the online methods was good; a total of 158 metabolites were identified. Using only the offline method, 156 (98.7%) metabolites were identified, while 151 (95.6%) were identified using only the online method. The metabolic pathways identified for the 11 cathinones included the reduction of the keto group, desalkylation, hydroxylation, and desmethylenation in cathinones containing a methylenedioxy moiety. Our method provides a straightforward approach to identifying metabolites which can then be added to the library utilized by our clinical toxicological screening method. The performance of our method compares well with that of an established offline HLM procedure, but is as automated as possible.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Re: Koko paperi -dumppaustopic
Kannabinoiditutkimuksen huippunimen Alexandros Makriyanniksen (AM-sarjan kehittäjä) ja kumppaneiden meta-analyyttinen yhteenveto erilaisten kannabinergisten aineiden fysiologisista vaikutuksista.
Cannabinergic ligands (Palmer SL, Thakur GA, Makriyannis A., 2002)
Cannabinergic ligands (Palmer SL, Thakur GA, Makriyannis A., 2002)
The understanding of the pharmacology surrounding the cannabinergic system has seen many advances since the discovery of the CB1 receptor in the mammalian brain and the CB2 receptor in the periphery. Among these advances is the discovery of the endogenous ligands arachidonoylethanolamide (anandamide) and 2-arachidonoylglycerol amide (2-AG), which are selective agonists for the CB1 and CB2 receptors, respectively. These endogenous neuromodulators involved in the cannabinergic system are thought to be produced on demand and are metabolized by the enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAG lipase). Recently, we characterized a reuptake system that facilitates the transport of anandamide across the cell membrane and subsequently developed selective inhibitors of this transport, which have been found to have therapeutic potential as analgesic and peripheral vasodilators. The cannabinergic proteins currently being explored, which include the CB1 and CB2 receptors, FAAH and the anandamide transporter, are excellent targets for the development of therapeutically useful drugs for a range of conditions including pain, loss of appetite, immunosuppression, peripheral vascular disease and motor disorders. As cannabinoid research has progressed, various potent and selective cannabimimetic ligands, targeting these four cannabinoid proteins, have been designed and synthesized. Many of these ligands serve as important molecular probes, providing structural information regarding the binding sites of the cannabinergic proteins, as well as pharmacological tools, which have been playing pivotal roles in research aimed at understanding the biochemical and physiological aspects of the endocannabinoid system. This review will focus on some of the current cannabinergic ligands and probes and their pharmacological and therapeutic potential.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Re: Koko paperi -dumppaustopic
Kannabinoidireseptoreja on nähtävästi muitakin kuin tunnistetut kaksi (CB1/2). GPR55:stä kaavaillaan CB3-reseptoria.
Novel cannabinoid receptors (Review) (A J Brown, 2007)
Novel cannabinoid receptors (Review) (A J Brown, 2007)
Cannabinoids have numerous physiological effects. In the years since the molecular identification of the G protein-coupled receptors CB1 and CB2, the ion channel TRPV1, and their corresponding endogenous ligand systems, many cannabinoid-evoked actions have been shown conclusively to be mediated by one of these specific receptor targets. However, there remain several examples where these classical cannabinoid receptors do not explain observed pharmacology. Studies using mice genetically deleted for the known receptors have confirmed the existence of additional targets, which have come to be known collectively as non-CB1/CB2 receptors. Despite intense research efforts, the molecular identity of these non-CB1/CB2 receptors remains for the most part unclear. Two orphan G protein-coupled receptors have recently been implicated as novel cannabinoid receptors; these are GPR119, which has been proposed as a receptor for oleoylethanolamide, and GPR55 which has been proposed as a receptor activated by multiple different cannabinoid ligands. In this review I will present an introduction to non-CB1/CB2 pharmacology, summarize information on GPR55 and GPR119 currently available, and consider their phylogenetic origin and what aspects of non-CB1/CB2 pharmacology, if any, they help explain.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Re: Koko paperi -dumppaustopic
Nagai F, Nonaka R, Satoh Hisashi Kamimura K.
The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.
Eur J Pharmacol. 2007 Mar 22;559(2-3):132-7. Epub 2006 Dec 12.
The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.
Eur J Pharmacol. 2007 Mar 22;559(2-3):132-7. Epub 2006 Dec 12.
We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. Alpha-metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-alpha-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines. N,N-dipropyltryptamine (DPT), 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-N,N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.
"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Mielenkiintoisia tiedeartikkeleita
Selective 5-HT2A agonist hallucinogens: A review of pharmacological interaction and corollary perceptual effects
Abstract/Summary
The most potent tryptamine hallucinogens – such as DMT, psilocybin, and LSD – are all active at the 5-HT2A receptor subtype and all produce similar visual perceptual results that are immediately recognizable as uniquely psychedelic. Although it is widely accepted that selective serotonin receptor subtype 2A agonism is directly responsible for producing the distinct hallucinations seen on a psychedelic trip, no single theory has yet explained why this is so.
Runaway Feedback Excitation and Multi-Stable Phase States
"The most important findings were increases in global EEG coherence in the 36-44 Hz and 50-64 Hz frequency bands for both subjects. Widely distributed cortical hyper-coherence seems reasonable given the intense synesthesia during ayahuasca experiences. Other findings include increased modal EEG alpha frequency and global power decreases across the cortex in most frequency bands... We believe that finding increases in global gamma coherence during peak psychedelic experiences might contribute to the discussion of binding theory. Also, in light of recent research with gamma coherence during advanced meditative conditions, our findings might further the comparison of shamanic psychedelic practices with meditation."
While this study demonstrates my point precisely, the science in this area is hardly conclusive. Depending of the type of EEG analysis performed, brainwave results from differing studies can have ambiguous results, like the following ayahuasca EEG study from Erik Hoffmann:
“Following three doses of the tea, the subjects showed strong and statistically significant increases of both EEG alpha (8-13Hz) and theta (4-8Hz) mean amplitudes compared to baseline while beta (13-20Hz) amplitudes were unchanged. The strongest increases of alpha activity were observed in the occipital lobes while alpha was unchanged in the frontal lobes. Theta amplitudes, on the other hand, were significantly increased in both occipital and frontal areas. Our data do not support previous findings of cortical activation with decreased alpha and increased beta activity caused by psychedelics”
While these conflicting EEG studies can be confounding, all of these findings demonstrate that 5-HT2A hallucinogens operate as phase-state drivers which can excite, disrupt, and resynchronize the intensity and global coherence of activity in the visual cortex.
Pulse-Driven Phase Coupling and Flashbacks
While the psychedelic flashback itself is an elusive beast, we know enough about it to make some assumptions based on the multi-state model presented here. Like déjà vu, the flashback is the instinctual subconscious recognition of a pattern or form which evokes hallucination or the hyper-coherent state of psychedelic consciousness. Assuming that various states of consciousness can be construed in terms of the pulse-driven couplings of various brain areas, it can be said that psychedelics “introduce” the brain to novel patterns of pulse-driven couplings, creating wholly novel and unique brain states. Once familiar with these new “psychedelic” brain patterns anything that evokes these patterns is instantly recognized as “psychedelic”, thus creating a memory or flashback of that unique archetypal state. The hyper-coherent phase-state created by psychedelics does not happen spontaneously in human consciousness (though the argument could be made in the case of sleep deprivation and extreme manic-psychosis), but the memory of that induced state may be enough to invoke a slight shift in waking phase state close enough to recall some small echo of the experience.
Persistent Psychedelic-Induced Delusional Psychosis
..the hard questions of what differentiates a robust psyche from a fragile psyche, and what actually “breaks” during the process of psychedelic activation. It could be argued that persistent overloading, decoupling, and “re-booting” of the entire cortex puts a strain on the network that, over time, degrades the brain’s ability to retain global cohesion in a normal waking state. This could be defined as a kind of network burnout resulting in scattered and un-focused personality disorders. If network burnout were the culprit, one would expect the results to be reversible through sustained abstinence, but since there are few studies in this area these speculations remain unresolved.
..
In psychedelic therapy the process of undoing maladaptive pathways is called “catharsis”; the process of wiring novel pathways out of the psychedelic experience is called “integration”. In psychedelic literature the process of doing this to the self is called “metaprogramming”. In each of these instances psychedelics are used to remove previous associations and re-train new beliefs and behaviors. If we are to take for granted that psychedelics facilitate this process of synaptic plasticity, then it must be presumed that this very process can be used to imprint and reinforce positive as well as delusional and maladaptive belief systems over time.
In the case of maladaptive psychedelic programming, one would expect to see the subject crafting self-referential occult belief systems based on ambiguous or archetypal symbols over a period of many months, weeks, or years. These occult belief systems would become more complex over time, relying on a hyper-articulated network of connections between language and symbol systems, thus creating eccentric logic pathways that grow so tangentially elaborate they eventually eclipse common rationality. A person suffering from this syndrome may also exhibit messianic or megalomaniacal tendencies, such as the belief that their occult system was derived from divine origin, along with the urgent need to spread a paradoxical prophecy of doom and transcendence. This syndrome is not symptomatic of neural damage or breakage, it is symptomatic of wholly unique logic pathways forged through obsessive self-referential feedback ideation, facilitated and reinforced through repeated high-dose application of selective 5-HT2A agonists.
Last edited by tRip on Tue 10 Jul 2012, 19:14, edited 1 time in total.
Reason: vaihdoin quotei
Reason: vaihdoin quotei
Keep it unreal.
Vaultti.net - coming soon..
Vaultti.net - coming soon..
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Re: Mielenkiintoisia tiedeartikkeleita
Multiple MDMA (Ecstasy) Overdoses at a Rave Event: A Case Series.
http://www.ncbi.nlm.nih.gov/pubmed/22640978
http://www.ncbi.nlm.nih.gov/pubmed/22640978
Looking for planet Gong...
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Re: Tutkimukset
HS: Huumetutkija: Diilerit syrjäyttivät ystävät
"Sosiologi Jussi Perälä vietti kymmenen vuotta Helsingin huumepiireissä tutkiessaan huumeiden käyttäjiä ja myyjiä. Sinä aikana diilereistä tuli ystäviä ja vanhat ihmissuhteet katkesivat. Arkeen oli ankeaa palata."
(Jussi Perälä: "Miksi lehmät pitää tappaa?" Etnografinen tutkimus 2000-luvun alun huumemarkkinoista Helsingissä)
"Sosiologi Jussi Perälä vietti kymmenen vuotta Helsingin huumepiireissä tutkiessaan huumeiden käyttäjiä ja myyjiä. Sinä aikana diilereistä tuli ystäviä ja vanhat ihmissuhteet katkesivat. Arkeen oli ankeaa palata."
(Jussi Perälä: "Miksi lehmät pitää tappaa?" Etnografinen tutkimus 2000-luvun alun huumemarkkinoista Helsingissä)
"Life is like stepping into a boat that is about to sail out to sea and sink." —Shunryu Suzuki
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Re: Tutkimukset
Mielenkiintoinen tutkimus: Tiedätkö miten parasetamoli vaikuttaa?
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Re: Tutkimukset
En löytänyt aiheesta aiempaa mainintaa haulla.
Ylen Ajankohtainen Kakkonen ohjelmassa oli eilen pätkää jätevesien huumausainejäämistä. Ei näyttänyt vielä olevan verkossa tuota jaksoa joten lisään tähän linkin Hesarin artikkeliin viime vuoden puolelta.
Pääasiat joita jäivät ohjelmasta mieleen olivat seuraavaa, ei ehkä mitenkään yllättävää tai uutta tietoa monellekaan;
- Suomessa käytetään huomattavia määriä amfetamiinia ja metamfetamiinia verrattuna läntiseen ja eteläiseen Eurooppaan.
- Kokaiinia ei Turussa esiinny miltei lainkaan, Helsingissä jonkun verran.
- Ekstaasin käyttö rajoittuu lähinnä viikonloppuihin.
- Pariiissa ei havaittu eroa kannabiksen käytössä eri asuinalueiden välillä. Käyttö oli samassa laajuudessa, oli kyseessä sitten paremmat kulmat tai köyhemmät kujat.
- Jos oikein muistan, niin sellainen luku jäi mieleen kuin n. 300mg metaa per asukas/vrk Etelä-Suomessa oli käytön laajuus tutkimuksen mukaan.
- Pystyisivät rajaamaan tutkimukseen miltei yksilötasolle, mutta eivät eettisistä syistä tätä tee.
- Vaikka tutkijat lupasivat täyden anonymiteetin, eivät ranskalaiset hiihtokeskukset halunneet lähteä tutkimukseen mukaan.
Tämä ylläoleva siis Ylen ohjelmasta, seuraava Hesarin artikkelista:
Ylen Ajankohtainen Kakkonen ohjelmassa oli eilen pätkää jätevesien huumausainejäämistä. Ei näyttänyt vielä olevan verkossa tuota jaksoa joten lisään tähän linkin Hesarin artikkeliin viime vuoden puolelta.
Pääasiat joita jäivät ohjelmasta mieleen olivat seuraavaa, ei ehkä mitenkään yllättävää tai uutta tietoa monellekaan;
- Suomessa käytetään huomattavia määriä amfetamiinia ja metamfetamiinia verrattuna läntiseen ja eteläiseen Eurooppaan.
- Kokaiinia ei Turussa esiinny miltei lainkaan, Helsingissä jonkun verran.
- Ekstaasin käyttö rajoittuu lähinnä viikonloppuihin.
- Pariiissa ei havaittu eroa kannabiksen käytössä eri asuinalueiden välillä. Käyttö oli samassa laajuudessa, oli kyseessä sitten paremmat kulmat tai köyhemmät kujat.
- Jos oikein muistan, niin sellainen luku jäi mieleen kuin n. 300mg metaa per asukas/vrk Etelä-Suomessa oli käytön laajuus tutkimuksen mukaan.
- Pystyisivät rajaamaan tutkimukseen miltei yksilötasolle, mutta eivät eettisistä syistä tätä tee.
- Vaikka tutkijat lupasivat täyden anonymiteetin, eivät ranskalaiset hiihtokeskukset halunneet lähteä tutkimukseen mukaan.
Tämä ylläoleva siis Ylen ohjelmasta, seuraava Hesarin artikkelista:
http://www.hs.fi/tiede/a1387334358341Jätevesi kertoo ihmisten kehon läpi kulkeneista aineista, myös huumeista. Aalto-yliopiston ja Helsingin yliopiston hanke kartoitti amfetamiinin, metamfetamiinin, ekstaasin, kokaiinin ja kannabiksen määriä suomalaisten kaupunkien jätevesissä. "Huumeiden määrä jätevesissä kertoo huumeiden käytöstä paremmin kuin kyselyt", kiteyttää Aalto-yliopiston vesihuoltotekniikan professori Riku Vahala.
"I think that in human evolution it has never been as necessary to have this substance LSD. It is just a tool to turn us into what we are supposed to be." -Albert Hoffman-
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Re: Tutkimukset
Iversen et al.
Neurochemical profiles of some novel psychoactive substances
DL: http://libgen.org/scimag/get.php?doi=10 ... 012.12.006
Eur J Pharmacol. Volume 700, Issues 1–3, 30 January 2013, Pages 147–151

Neurochemical profiles of some novel psychoactive substances
DL: http://libgen.org/scimag/get.php?doi=10 ... 012.12.006
Eur J Pharmacol. Volume 700, Issues 1–3, 30 January 2013, Pages 147–151
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.

"Jos ihmismieli on ihmeellisin asia mitä maa päällään kantaa, pyrkimys tutkia narkoottisten ja stimuloivien aineiden psykofysiologisen vaikutuksen syvyyksiä saa tämän ihmeen vaikuttamaan vieläkin suuremmalta."
— Professori Louis Lewin, 1924
— Professori Louis Lewin, 1924
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Re: Mielenkiintoisia tiedeartikkeleita
Ajattelin, että tälläne on hyvä laittaa ilmoille http://www.ncbi.nlm.nih.gov/pubmed/24590542. Vaikka varmasti jokaselle yleisesti tiedossa, että MDMA tuhoaa neuroneita (onhan?), niin tää reviewi sai allekirjoittaneen pohtimaan omaa käyttöä. En sillä, että varmastikaan lopettaisin käytön, mutta ainaki harvemmalla aikavälillä tästä eteenpäin.
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Re: Tutkimusjulkaisut
Väitöskirja muuntohuumeista: http://urn.fi/URN:ISBN:978-951-51-0550-9
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Re: Tutkimusjulkaisut
Drugs as risks in cold exposure
Alcohol
Alcohol is the most frequent risk drug concerning cold exposure especially in young healthy persons causing hypothermia even temperate climate. The severity of the risk depends mainly on the blood alcohol concentration,but other factors ,such as fasting,physical exercise and old age can increase the risk further.In cases of fatal or near fatal accidental hypothermia blood alcohol concentration has been over 1g/100 ml (0.1 %), usually around 0.2 %.
Alcohol has some pharmacological effects ,which increase the tendency of lowering body temperature in cold environment.Alcohol depresses the central thermoregulatory center,and diminishes the uncomfortable or painful sense of cold . It also dilates the cutaneous vessels thus increasing loss of body heat through the skin. Alcohol also prevents shivering and has hypoglycaemic and antiketonaemic effects thus decreasing heat production.The diuretic and vasodilating effect of alcohol may lead to smaller blood volume and thus lowers blood pressure and cerebral circulation.
Small amounts of alcohol,blood alcohol concentration around 0.05 % seem not to be risky and theoretically one might benefit from the high energy content of ethanol in the heat production.Furthermore the vasodilating effect is weaker and vasoconstriction caused by cold air or cold water prevails. However,even small dosis of alcohol together with physical exercise can cause
unexpected drop of body temperature probably through hypoglycaemia.
Quite controversially alcohol has been found to prevent death in very deep hypothermia by
preventing cardiac fibrillation below 27 oC of body temperature.Ashtonishing survivals of persons
with core temperature of 20oChave been reported,but severe frostbites occurred in these victims.
Other drugs
Neuroleptics are a group of medicines which have been found in victims of hypothermia.Phenothiazines,even in therapeutic doses are considered to have depressive effect on central thermoregulation mechanisms followed by diminished sensation to cold and turning the person indolent.Combinations of psychothrophic drugs have been observed to cause unexpected decrease of body temperature even in mild cold.The risk connected with neuroleptics has been shown also in animal experiments.
Tranquilizers such as benzodiazepines and buspirone have also been found in hypothermia victims and animal experiments have shown their impairing effect to withstand severe cold.Their mode of effect is likely mediated through central thermoregulation (effect on setpoint) and behaviour.
Barbiturates,rarely used nowadays,,are considered to have depressing effect on central thermoregulation and to alter proper behaviour in cold. Opiates seem to have similar,though milder risks for hypothermia.
Tricyclic and other antidepressants are widely used drugs, but they seem to have no observable risk concerning hypothermia.Similarly beta-blockers seem to be quite safe considering thermoregulation.