Tema: 25C-NBOMe: Preliminary Data on Pharmacology, Psychoactive Effects, and Toxicity

Página 1 de 2 12 ÚltimoÚltimo
Resultados 1 al 10 de 16
  1. #1
    Un Viejo Conocido Avatar de Yyy
    Ubicación
    Hiperespacio
    Mensajes
    1,270

    25C-NBOMe: Preliminary Data on Pharmacology, Psychoactive Effects, and Toxicity

    Les dejo algunas partes, el paper completo al final. Es nuevito

    Abstract

    Introduction. The use of novel psychoactive substances (NPSs) has rapidly increased as well as their online availability. The aim of this paper is to provide a comprehensive review of the nature and the risks associated with 25C-NBOMe, which has recently appeared in the drug market. Methods. A systematic analysis of the scientific literature and a qualitative assessment of online and media resources (e.g., e-newsgroups, chat-rooms, and e-newsletters) in 10 languages were carried out. Results. 25C-NBOMe is sold online as legal LSD or as research chemical with different designations such as “Boom,” “Pandora,” “Holland film,” or “N-bomb.” It is a partial agonist of 5-HT2A receptors. It is usually ingested orally/sublingually and, less commonly, nasally, through injection, vaginally, rectally, and smoked. Its effects include sublingual numbing, stimulation, “body high,” hallucinations, dissociation, and anxiety. 25C-NBOMe presents high risk of overdoses; acute toxicity and fatalities have been reported. Conclusions. 25C-NBOMe consumption represents an emerging phenomenon with potential harmful effects. Its use is increased by its online availability at low costs. Health and other professionals should be informed about this new trend of substance use.
    Results

    3.1. 25C-NBOMe: An Emerging Hallucinogenic Substance in the Drug Market

    25C-NBOMe, also known as NBOMe-2CC, Boom, C-Boom, Cimbi-82, Pandora, N-bomb, Holland film, and Dime [12], has been first synthesized in 2009 and first mentioned in the scientific literature in 2011 by Ettrup et al. [13, 14]. To our knowledge, the first case of 25C-NBOMe ingestion was recordedin 2010 [15]. The drug is believed to be manufactured in China, but shipments from Europe and Canada have also been reported [5].

    25C-NBOMe is a N-(2-methoxy)benzyl derivative of the psychedelic phenethylamine 2C-C (4-chloro-2,5-dimethoxyphenethylamine) [16] (Figure 1). It is derived from 2C-C by substitution on the amine nitrogen with a 2-methoxybenzyl (BOMe) group. 2C-C belongs to a group of modified phenethylamine structures called dimethoxyphenyl-ethanamines, also known as 2C substitutes [16]. The terminology “2C” was created by Alexander Shulgin et al. to describe the two carbons between the amino group and the benzene ring in the chemical structure [6, 16]. The 2-methoxybenzyl group attached at a nitrogen atom in 25C-NBOMe acts as protecting group in order to preserve the functionality of the amine group during a reaction [12, 16]. This structural change allows a 16-fold increase in potency as compared to other NBOMe compounds [16].

    3.2 Pharmacology

    The pharmacological properties of NBOMe series were first investigated by Heim and collaborators [17]. 25C-NBOMe acts as a potent partial agonist for the 5-HT2A receptor and has been studied in its 11C radiolabelled form as a potential ligand for mapping the distribution of 5-HT2A receptors in the brain using positron emission tomography (PET) [13].

    25C-NBOMe is characterized by nanomolar affinity towards the 5-HT2A receptor and has an agonistic binding affinity of ?nM in vitro [13]; consistently, it has been described by Braden et al. as “superpotent” agonist of the 5-HT2A receptors [18] and it is pharmacologically active even at very low submilligram doses [16].

    3.4. Route of Administration and Dosage

    25C-NBOMe can be consumed through several routes of administration. The most common route of administration is the oral or sublingual ingestion (mixed with solvents such as alcohol) by soaking the liquid on a blotter and keeping it on the buccal mucosa for several minutes or swallowing it; Lawn et al. undertook a survey study through the Global Drugs Survey reporting that 81.2% of users administered the drug orally or sublingually [20]. Less commonly, 25C-NBOMe can be taken nasally (insufflation and absorption of liquid solutions), through injection (intravenously and intramuscularly), vaginally, and rectally, and it can be smoked as freebase [12, 20, 21].

    Several independent reports suggest that doses of swallowed 25C-NBOMe range between 50 and 1200??g and that hallucinogenic effects can be achieved at a dose of 50–200??g [12, 15, 21]. When administered sublingually, the threshold for the onset of hallucinogenic effects reportedly is about 100–250??g, with mild effects after 250–450??g, strong after 450–800??g, and very strong over 800??g [12]. The effects of insufflated 25C-NBOMe have been described as light after 50–200??g, mild after 200–350??g, strong after 350–700??g, and very strong after higher doses [12]. Finally, several independent users report to smoke the substance dissolving 10?mg of 25C-NBOMe freebase in 30?mL 99.9% isopropanol and then to dry 1?mL “doses” (300??g) onto plant matter to be smoked in cigarettes or pipes; in this latter case, the threshold for the onset of intense hallucinogenic effects is about 50–200??g [22].

    Example doses reported on the drug fora involving more rare routes of administration include “830??g, injected,” “400??g, rectally,” and “500??g, vaginally” [21, 23, 24].

    3.5. Effects

    (i) Sublingual Numbness. When taken sublingually, the first effects are anecdotally described as unpleasant. These include a metallic chemical taste along with a sense of numbness of the tongue and mouth, which can last up to an hour after the ingestion. Numbness of the tongue and mouth has been reported to be a key difference between blotter papers containing LSD and those containing NBOMe drugs [25].

    (ii) Body High. The “body high” can be described as a generally mild, all-encompassing, soft but euphoric tingling sensation. This tingling sensation is also accompanied by spontaneous rushes of euphoria which become longer and more drawn out proportional to the dosage consumed [12, 25].

    (iii) Stimulation. 25C-NBOMe can have stimulants effects. According to subjective reports, it generates a “unique” sense of stimulation, which has been described as “energetic” but at the same time devoid of any physical movement, unless intentional. For some users, the stimulation can be quite uncontrollable, occasionally resulting in bodily shakes and a grinding of the teeth comparable to that of MDMA and traditional stimulants such as amphetamine [12, 25].

    (iv) Psychedelic Effects. They can differ significantly. These include introspection, euphoria, acceleration of thought, conceptual thinking, time distortion, increased empathy, and sociability. Other effects, which become more common as dosages increase, include depersonalization, derealization, anxiety, dissociation, panic, and fear [25]. In addition, 25C-NBOMe is able to cause a wide range of hallucinatory states, including visual and auditory hallucinations [12, 25]. Visual effects of the drug include increased visual acuity, enhanced pattern recognition, enhanced colors, and distortions (e.g., visual drifting, texture repetition, and tracers) [12, 25]. A summary of 25C-NBOMe effects is given in Table 1.

    3.6. Toxicity

    Common negative physical side effects of 25C-NBOMe include vasoconstriction, nausea, vomiting, headache, irregular heartbeat, sweating, and temporary dysuria [4, 25, 27]; some users anecdotally reported to have experienced “something terrifying to the body” after its consumption [26]. Overdoses lead to most severe effects; some recently reported cases of intoxication were associated with confusion, agitation, hypertension, tachycardia, hyperthermia, dilated pupils, heart failure, metabolic acidosis, generalized seizure, loss of consciousness, low oxygen saturation, acute kidney, and lung failures [25, 27–29].

    As 25C-NBOMe is a potent serotonergic agonist, these toxic effects may represent the clinical manifestations of serotonin toxidrome, which is known to potentially produce acute toxicity involving metabolic acidosis, rhabdomyolysis, seizures, renal failure, and disseminated intravascular coagulation.

    25C-NBOMe is strongly active at extremely small doses (it exerts its effects even at microgramic levels) and users may not have precise weighing scale; therefore, the possibility of accidental overdoses is not irrelevant. In addition, the lack of knowledge of an experimentally recognized median lethal dosage (LD50), the frequent poor or mistaken dilution, and the improper handlings especially by teenagers (including the concomitant use with other drugs like methoxetamine, ?-methyltryptamine, or synthetic cannabinoids) contribute to increase the risk of accidental overdoses of the substance and related deaths [28, 29].

    Since June 2012, more than 10 fatalities have been reported as a result of the ingestion of substances in the NBOMe class [4, 27, 30–32] and at least 2 of these were attributable to 25C-NBOMe; in 2013, a 16-year-old and an 18-year-old males died in USA and UK after having inhaled the drug [9, 21, 25].
    Fuente

  2. #2
    Señor Miembro Avatar de jorjos Conocido
    Ubicación
    Buenos Aires
    Mensajes
    180
    Muy buena info, me hubiese gustado que explique que tan seguido y por que lapso de tiempo hay que consumir NBOMe para que se den los efectos negativos que se mencionan, igualmente con esto ya se puede ver que es una sustancia mas nociva a nivel salud que el LSD.
    Última edición por jorjos; 09/07/2014 a las 10:52

  3. #3
    Agonista parcial? Ja, contate otro! Más total imposible.

  4. #4
    Cita Iniciado por Mr. Chemistry Ver mensaje
    Agonista parcial? Ja, contate otro! Más total imposible.
    Que sea parcial o total cambia algo en el efecto u otra cosa? No se mucho de farmaco, pero nunca entendí porque algunas sustancias que actúan en el mismo receptor tienen efectos tan distintos

  5. #5
    Creo que se entiende que eso no es nada serio. -.-

  6. #6
    Un Viejo Conocido Avatar de Morfeo Conocido
    Mensajes
    790
    Cita Iniciado por Godislove Ver mensaje
    Creo que se entiende que eso no es nada serio. -.-
    Como que no? Es un paper...

  7. #7
    Un Viejo Conocido Avatar de Yyy
    Ubicación
    Hiperespacio
    Mensajes
    1,270
    Cita Iniciado por Mr. Chemistry Ver mensaje
    Agonista parcial? Ja, contate otro! Más total imposible.
    Si tenes biblio para contrastar, bienvenido sea

    Cita Iniciado por Godislove Ver mensaje
    Creo que se entiende que eso no es nada serio. -.-
    Lo mismo que morfeo, por que no? Ojo, que sea un paper no le da autoridad absoluta, eso es seguro, pero tenes el paper entero para leerlo y criticar lo metodos utilizados, interpretacion de los resultados o las referencias para ver que tan confiable son. En base a eso podes argumentar vos por que no es serio (citando tus fuentes, claro). Decirlo al boleo es nada.

    El titulo del mismo es bien claro, Preliminary Data (...).

    En fin, argumenten

  8. #8
    Cita Iniciado por Yyy Ver mensaje
    Si tenes biblio para contrastar, bienvenido sea
    Tenés acceso a papers? No puedo encontrar el de Ettrup que citan en todos lados, "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers".

    Igualmente, encontré otro que cita los datos que necesito:

    http://www.who.int/medicines/areas/q..._18_review.pdf

    Y dice:

    Binding (Ki) at the rat 5-HT2A receptor was reported to be 2.89±1.05 nM with activation (ED50) of 2.31±0.11 nM and intrinsic activity of 88% (Ettrup et al., 2011).
    Técnicamente si no llega al 100% de eficacia no es total, pero en la práctica no hay diferencia. La del 25I creo haberla leído en algún lado, si mal no recuerdo era de 91%. Al 25C lo pintan como muchísimo más seguro cuando en realidad no es más que juego de tecnicismos.
    Actividad intrínseca del LSD en 5-HT2A no tenés idea? Como para comparar.

  9. #9
    Un Viejo Conocido Avatar de Gisoma
    Ubicación
    Fuera de tu alcance
    Mensajes
    785
    Cita Iniciado por Mr. Chemistry Ver mensaje
    Tenés acceso a papers? No puedo encontrar el de Ettrup que citan en todos lados, "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers".

    Igualmente, encontré otro que cita los datos que necesito:

    http://www.who.int/medicines/areas/q..._18_review.pdf

    Y dice:



    Técnicamente si no llega al 100% de eficacia no es total, pero en la práctica no hay diferencia. La del 25I creo haberla leído en algún lado, si mal no recuerdo era de 91%. Al 25C lo pintan como muchísimo más seguro cuando en realidad no es más que juego de tecnicismos.
    Actividad intrínseca del LSD en 5-HT2A no tenés idea? Como para comparar.

    el 25c es muchisimo mas seguro y tranquilo, tendrias que probarlo para liberarte de tanto escepticismo.
    creo en el karma en el dharma en la energia y en la magia.

  10. #10
    Cita Iniciado por Gisoma Ver mensaje
    el 25c es muchisimo mas seguro y tranquilo, tendrias que probarlo para liberarte de tanto escepticismo.
    Poniendo en la balanza los pro y los contra no veo buen pronóstico como para probarlo. Ni ese ni otros NBOMe. Prefiero confiar en lo que me contó gente de confianza y debatir sobre los números.

Permisos de publicación

  • No puedes crear nuevos temas
  • No puedes responder temas
  • No puedes subir archivos adjuntos
  • No puedes editar tus mensajes
  •