The Experts below are selected from a list of 222 Experts worldwide ranked by ideXlab platform
John Mendelson - One of the best experts on this subject based on the ideXlab platform.
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Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial
Psychopharmacology, 2011Co-Authors: John Mendelson, Jeremy R. Coyle, Juan Carlos Lopez, Matthew J. Baggott, Keith Flower, E. Thomas Everhart, Thomas A. Munro, Gantt P. Galloway, Bruce M. CohenAbstract:Rationale Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused Hallucinogenic Plant. Objectives The objectives of this study were to characterize the physiological and subjective effects of SA versus placebo and measure drug and metabolite levels. Methods Sublingual SA doses up to 4 mg were administered in dimethyl sulfoxide/polyethylene glycol 400 solution to eight SD-experienced subjects using a placebo-controlled ascending-dose design. Results No dose of SA produced significantly greater physiological or subjective effects than placebo. Furthermore, effects did not resemble reported “typical” effects of smoked SD. SA was detectable in plasma and urine, but was, in most cases, below the reliable limit of quantification (0.5 ng/mL). Conclusions Our results suggest that the sublingual bioavailability of SA is low. Higher doses, alternate formulations, or alternate routes of administration will be necessary to study the effects of SA in humans.
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Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial
Psychopharmacology, 2010Co-Authors: John Mendelson, Jeremy R. Coyle, Juan Carlos Lopez, Matthew J. Baggott, Keith Flower, E. Thomas Everhart, Thomas A. Munro, Gantt P. Galloway, Bruce M. CohenAbstract:Rationale Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused Hallucinogenic Plant.
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use of salvia divinorum an unscheduled Hallucinogenic Plant a web based survey of 500 users
Clinical Pharmacology & Therapeutics, 2004Co-Authors: Matthew J. Baggott, Earth Erowid, Fire Erowid, John MendelsonAbstract:Salvia divinorum (SD) is a legal psychoactive Plant that produces hallucinogen-like effects through a putative kappa opiate mechanism. We characterized the reasons, methods, and reported consequences of SD use in a sample of 500 users (92.6% male, 23.4±8.7, range 13–68 years) with an on-line questionnaire. They had used 13.3±22.9 (range 1–250) times, usually to explore altered consciousness or to have a spiritual/mystical experience. 80.6% probably or definitely would use SD again. 92.6% smoked SD with 61.4% using a concentrated extract and 37.3% using dried leaf; effects were estimated to last 14.1±12.8 minutes. Compared to other methods of altering consciousness, SD effects were felt to be unique. Common (>25%) after-effects of SD included feelings of increased insight (47%), improved mood (44.8%), calmness (42.2%), increased sense of connection with the universe or nature (39.8%), weird thoughts (36.4%), things seem unreal (32.4%), floating feeling (32%), increased sweating (28.2%) and body felt warm or hot (25.2%). 25.8% reported persisting (>24 hr) positive effects (usually an increased sense of well-being) on at least 1 occasion. 4.4% had persisting negative effects (most often anxiety). 0.6% had sought professional help for a SD-related problem. At some point, 0.6% felt addicted to or dependent upon SD; 1.2% reported strong cravings for SD; 0.4% endorsed three DSM-IV dependence criteria. We conclude that SD is commonly used and merits further study. Clinical Pharmacology & Therapeutics (2004) 75, P72–P72; doi: 10.1016/j.clpt.2003.11.270
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Use of salvia divinorum, an unscheduled Hallucinogenic Plant: a web‐based survey of 500 users
Clinical Pharmacology & Therapeutics, 2004Co-Authors: Matthew J. Baggott, Earth Erowid, Fire Erowid, John MendelsonAbstract:Salvia divinorum (SD) is a legal psychoactive Plant that produces hallucinogen-like effects through a putative kappa opiate mechanism. We characterized the reasons, methods, and reported consequences of SD use in a sample of 500 users (92.6% male, 23.4±8.7, range 13–68 years) with an on-line questionnaire. They had used 13.3±22.9 (range 1–250) times, usually to explore altered consciousness or to have a spiritual/mystical experience. 80.6% probably or definitely would use SD again. 92.6% smoked SD with 61.4% using a concentrated extract and 37.3% using dried leaf; effects were estimated to last 14.1±12.8 minutes. Compared to other methods of altering consciousness, SD effects were felt to be unique. Common (>25%) after-effects of SD included feelings of increased insight (47%), improved mood (44.8%), calmness (42.2%), increased sense of connection with the universe or nature (39.8%), weird thoughts (36.4%), things seem unreal (32.4%), floating feeling (32%), increased sweating (28.2%) and body felt warm or hot (25.2%). 25.8% reported persisting (>24 hr) positive effects (usually an increased sense of well-being) on at least 1 occasion. 4.4% had persisting negative effects (most often anxiety). 0.6% had sought professional help for a SD-related problem. At some point, 0.6% felt addicted to or dependent upon SD; 1.2% reported strong cravings for SD; 0.4% endorsed three DSM-IV dependence criteria. We conclude that SD is commonly used and merits further study. Clinical Pharmacology & Therapeutics (2004) 75, P72–P72; doi: 10.1016/j.clpt.2003.11.270
Mary Jeanne Kreek - One of the best experts on this subject based on the ideXlab platform.
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the widely available Hallucinogenic Plant salvia divinorum and its main component salvinorin a a unique κ opioid receptor kop r agonist with powerful behavioral and neurobiological effects
Neuropathology of Drug Addictions and Substance Misuse#R##N#Volume 2: Stimulants Club and Dissociative Drugs Hallucinogens Steroids Inhalants and Inte, 2016Co-Authors: Eduardo R Butelman, Mary Jeanne KreekAbstract:Abstract Salvia divinorum is a Hallucinogenic Plant originally used in traditional ethnomedical practice in certain cultures, but is now widely available in the industrialized world through a variety of sources. The main active component of Salvia divinorum is salvinorin A, a diterpene shown to be a selective high-efficacy κ-opioid receptor (KOP-r) agonist, without affinity for the site of action of classic hallucinogens (the 5-HT 2A receptor). Preparations containing salvinorin A cause robust but short-lasting visual and proprioceptive hallucinations, with commonly reported dissociative effects. These effects may be qualitatively similar to previously reported “psychotomimetic” effects observed in humans with synthetic KOP-r agonists. In preclinical animal models, salvinorin A produces behavioral and neurobiological effects qualitatively similar to those observed with synthetic KOP-r agonists. These effects include a decrease in dopaminergic activation. Activation of KOP-r receptors by synthetic and endogenous neuropeptide agonists (the dynorphins) are known to exert a negative modulatory function on dopaminergic systems. Other salvinorin A–induced effects (similar to those of KOP-r agonists) include aversion, anhedonia, and depressant-like and sedative like-effects. Furthermore, salvinorin A also produces robust prolactin release, a neuroendocrine biomarker measure previously used to study KOP-r agonist effects in humans.
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The Plant-derived hallucinogen, salvinorin A, produces κ-opioid agonist-like discriminative effects in rhesus monkeys
Psychopharmacology, 2004Co-Authors: Eduardo R Butelman, Todd J. Harris, Mary Jeanne KreekAbstract:Rationale Salvinorin A is the active component of the Hallucinogenic Plant Salvia divinorum. The potential mode of action of this hallucinogen was unknown until recently. A recent in vitro study detected high affinity and efficacy of salvinorin A at κ-opioid receptors. It was postulated that salvinorin A would produce discriminative stimulus effects similar to those of a high efficacy κ-agonist (U69,593) in rhesus monkeys. Methods Monkeys were previously trained to discriminate U69,593 (0.0056 or 0.013 mg/kg; SC) from vehicle in a food-reinforced FR20 (fixed ratio 20) operant conditioning procedure ( n =3). The ability of salvinorin A to cause generalization (≥90% U69,593-appropriate responding) was examined in time course and cumulative dose-effect curve studies. Results All subjects dose-dependently emitted full U69,593-appropriate responding after salvinorin A (0.001–0.032 mg/kg, SC). Salvinorin A-induced generalization started 5–15 min after injection, and dissipated by 120 min. The opioid antagonist quadazocine (0.32 mg/kg) fully blocked the effects of salvinorin A. The κ-selective antagonist GNTI (1 mg/kg; 24 h pretreatment) did not cause significant antagonism of the effects of salvinorin A (GNTI, under these conditions, was only effective as an antagonist in two of three monkeys). The NMDA antagonist ketamine (0.1–3.2 mg/kg) was not generalized by any subject, indicating that not all compounds that produce Hallucinogenic or psychotomimetic effects in humans are generalized by subjects trained to discriminate U69,593. Conclusions The naturally occurring hallucinogen salvinorin A produces discriminative stimulus effects similar to those of a high efficacy κ-agonist in non-human primates.
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The Plant-derived hallucinogen, salvinorin A, produces κ-opioid agonist-like discriminative effects in rhesus monkeys
Psychopharmacology, 2003Co-Authors: Eduardo R Butelman, Todd J. Harris, Mary Jeanne KreekAbstract:Rationale Salvinorin A is the active component of the Hallucinogenic Plant Salvia divinorum. The potential mode of action of this hallucinogen was unknown until recently. A recent in vitro study detected high affinity and efficacy of salvinorin A at κ-opioid receptors. It was postulated that salvinorin A would produce discriminative stimulus effects similar to those of a high efficacy κ-agonist (U69,593) in rhesus monkeys.
Matthew J. Baggott - One of the best experts on this subject based on the ideXlab platform.
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Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial
Psychopharmacology, 2011Co-Authors: John Mendelson, Jeremy R. Coyle, Juan Carlos Lopez, Matthew J. Baggott, Keith Flower, E. Thomas Everhart, Thomas A. Munro, Gantt P. Galloway, Bruce M. CohenAbstract:Rationale Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused Hallucinogenic Plant. Objectives The objectives of this study were to characterize the physiological and subjective effects of SA versus placebo and measure drug and metabolite levels. Methods Sublingual SA doses up to 4 mg were administered in dimethyl sulfoxide/polyethylene glycol 400 solution to eight SD-experienced subjects using a placebo-controlled ascending-dose design. Results No dose of SA produced significantly greater physiological or subjective effects than placebo. Furthermore, effects did not resemble reported “typical” effects of smoked SD. SA was detectable in plasma and urine, but was, in most cases, below the reliable limit of quantification (0.5 ng/mL). Conclusions Our results suggest that the sublingual bioavailability of SA is low. Higher doses, alternate formulations, or alternate routes of administration will be necessary to study the effects of SA in humans.
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Lack of effect of sublingual salvinorin A, a naturally occurring kappa opioid, in humans: a placebo-controlled trial
Psychopharmacology, 2010Co-Authors: John Mendelson, Jeremy R. Coyle, Juan Carlos Lopez, Matthew J. Baggott, Keith Flower, E. Thomas Everhart, Thomas A. Munro, Gantt P. Galloway, Bruce M. CohenAbstract:Rationale Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused Hallucinogenic Plant.
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use of salvia divinorum an unscheduled Hallucinogenic Plant a web based survey of 500 users
Clinical Pharmacology & Therapeutics, 2004Co-Authors: Matthew J. Baggott, Earth Erowid, Fire Erowid, John MendelsonAbstract:Salvia divinorum (SD) is a legal psychoactive Plant that produces hallucinogen-like effects through a putative kappa opiate mechanism. We characterized the reasons, methods, and reported consequences of SD use in a sample of 500 users (92.6% male, 23.4±8.7, range 13–68 years) with an on-line questionnaire. They had used 13.3±22.9 (range 1–250) times, usually to explore altered consciousness or to have a spiritual/mystical experience. 80.6% probably or definitely would use SD again. 92.6% smoked SD with 61.4% using a concentrated extract and 37.3% using dried leaf; effects were estimated to last 14.1±12.8 minutes. Compared to other methods of altering consciousness, SD effects were felt to be unique. Common (>25%) after-effects of SD included feelings of increased insight (47%), improved mood (44.8%), calmness (42.2%), increased sense of connection with the universe or nature (39.8%), weird thoughts (36.4%), things seem unreal (32.4%), floating feeling (32%), increased sweating (28.2%) and body felt warm or hot (25.2%). 25.8% reported persisting (>24 hr) positive effects (usually an increased sense of well-being) on at least 1 occasion. 4.4% had persisting negative effects (most often anxiety). 0.6% had sought professional help for a SD-related problem. At some point, 0.6% felt addicted to or dependent upon SD; 1.2% reported strong cravings for SD; 0.4% endorsed three DSM-IV dependence criteria. We conclude that SD is commonly used and merits further study. Clinical Pharmacology & Therapeutics (2004) 75, P72–P72; doi: 10.1016/j.clpt.2003.11.270
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Use of salvia divinorum, an unscheduled Hallucinogenic Plant: a web‐based survey of 500 users
Clinical Pharmacology & Therapeutics, 2004Co-Authors: Matthew J. Baggott, Earth Erowid, Fire Erowid, John MendelsonAbstract:Salvia divinorum (SD) is a legal psychoactive Plant that produces hallucinogen-like effects through a putative kappa opiate mechanism. We characterized the reasons, methods, and reported consequences of SD use in a sample of 500 users (92.6% male, 23.4±8.7, range 13–68 years) with an on-line questionnaire. They had used 13.3±22.9 (range 1–250) times, usually to explore altered consciousness or to have a spiritual/mystical experience. 80.6% probably or definitely would use SD again. 92.6% smoked SD with 61.4% using a concentrated extract and 37.3% using dried leaf; effects were estimated to last 14.1±12.8 minutes. Compared to other methods of altering consciousness, SD effects were felt to be unique. Common (>25%) after-effects of SD included feelings of increased insight (47%), improved mood (44.8%), calmness (42.2%), increased sense of connection with the universe or nature (39.8%), weird thoughts (36.4%), things seem unreal (32.4%), floating feeling (32%), increased sweating (28.2%) and body felt warm or hot (25.2%). 25.8% reported persisting (>24 hr) positive effects (usually an increased sense of well-being) on at least 1 occasion. 4.4% had persisting negative effects (most often anxiety). 0.6% had sought professional help for a SD-related problem. At some point, 0.6% felt addicted to or dependent upon SD; 1.2% reported strong cravings for SD; 0.4% endorsed three DSM-IV dependence criteria. We conclude that SD is commonly used and merits further study. Clinical Pharmacology & Therapeutics (2004) 75, P72–P72; doi: 10.1016/j.clpt.2003.11.270
Eduardo R Butelman - One of the best experts on this subject based on the ideXlab platform.
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the widely available Hallucinogenic Plant salvia divinorum and its main component salvinorin a a unique κ opioid receptor kop r agonist with powerful behavioral and neurobiological effects
Neuropathology of Drug Addictions and Substance Misuse#R##N#Volume 2: Stimulants Club and Dissociative Drugs Hallucinogens Steroids Inhalants and Inte, 2016Co-Authors: Eduardo R Butelman, Mary Jeanne KreekAbstract:Abstract Salvia divinorum is a Hallucinogenic Plant originally used in traditional ethnomedical practice in certain cultures, but is now widely available in the industrialized world through a variety of sources. The main active component of Salvia divinorum is salvinorin A, a diterpene shown to be a selective high-efficacy κ-opioid receptor (KOP-r) agonist, without affinity for the site of action of classic hallucinogens (the 5-HT 2A receptor). Preparations containing salvinorin A cause robust but short-lasting visual and proprioceptive hallucinations, with commonly reported dissociative effects. These effects may be qualitatively similar to previously reported “psychotomimetic” effects observed in humans with synthetic KOP-r agonists. In preclinical animal models, salvinorin A produces behavioral and neurobiological effects qualitatively similar to those observed with synthetic KOP-r agonists. These effects include a decrease in dopaminergic activation. Activation of KOP-r receptors by synthetic and endogenous neuropeptide agonists (the dynorphins) are known to exert a negative modulatory function on dopaminergic systems. Other salvinorin A–induced effects (similar to those of KOP-r agonists) include aversion, anhedonia, and depressant-like and sedative like-effects. Furthermore, salvinorin A also produces robust prolactin release, a neuroendocrine biomarker measure previously used to study KOP-r agonist effects in humans.
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The Plant-derived hallucinogen, salvinorin A, produces κ-opioid agonist-like discriminative effects in rhesus monkeys
Psychopharmacology, 2004Co-Authors: Eduardo R Butelman, Todd J. Harris, Mary Jeanne KreekAbstract:Rationale Salvinorin A is the active component of the Hallucinogenic Plant Salvia divinorum. The potential mode of action of this hallucinogen was unknown until recently. A recent in vitro study detected high affinity and efficacy of salvinorin A at κ-opioid receptors. It was postulated that salvinorin A would produce discriminative stimulus effects similar to those of a high efficacy κ-agonist (U69,593) in rhesus monkeys. Methods Monkeys were previously trained to discriminate U69,593 (0.0056 or 0.013 mg/kg; SC) from vehicle in a food-reinforced FR20 (fixed ratio 20) operant conditioning procedure ( n =3). The ability of salvinorin A to cause generalization (≥90% U69,593-appropriate responding) was examined in time course and cumulative dose-effect curve studies. Results All subjects dose-dependently emitted full U69,593-appropriate responding after salvinorin A (0.001–0.032 mg/kg, SC). Salvinorin A-induced generalization started 5–15 min after injection, and dissipated by 120 min. The opioid antagonist quadazocine (0.32 mg/kg) fully blocked the effects of salvinorin A. The κ-selective antagonist GNTI (1 mg/kg; 24 h pretreatment) did not cause significant antagonism of the effects of salvinorin A (GNTI, under these conditions, was only effective as an antagonist in two of three monkeys). The NMDA antagonist ketamine (0.1–3.2 mg/kg) was not generalized by any subject, indicating that not all compounds that produce Hallucinogenic or psychotomimetic effects in humans are generalized by subjects trained to discriminate U69,593. Conclusions The naturally occurring hallucinogen salvinorin A produces discriminative stimulus effects similar to those of a high efficacy κ-agonist in non-human primates.
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The Plant-derived hallucinogen, salvinorin A, produces κ-opioid agonist-like discriminative effects in rhesus monkeys
Psychopharmacology, 2003Co-Authors: Eduardo R Butelman, Todd J. Harris, Mary Jeanne KreekAbstract:Rationale Salvinorin A is the active component of the Hallucinogenic Plant Salvia divinorum. The potential mode of action of this hallucinogen was unknown until recently. A recent in vitro study detected high affinity and efficacy of salvinorin A at κ-opioid receptors. It was postulated that salvinorin A would produce discriminative stimulus effects similar to those of a high efficacy κ-agonist (U69,593) in rhesus monkeys.
Daniel E. Brooks - One of the best experts on this subject based on the ideXlab platform.
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Ayahuasca Exposure: Descriptive Analysis of Calls to US Poison Control Centers from 2005 to 2015
Journal of Medical Toxicology, 2017Co-Authors: C. William Heise, Daniel E. BrooksAbstract:Background Ayahuasca is a Hallucinogenic Plant preparation which usually contains the vine Banisteriopsis caapi and the shrub Psychotria viridis. This tea originates from the Amazon Basin where it is used in religious ceremonies. Because interest in these religious groups spreading as well as awareness of use of ayahuasca for therapeutic and recreational purposes, its use is increasing. Banisteriopsis caapi is rich in β-carbolines, especially harmine, tetrahydroharmine and harmaline, which have monoamine oxidase inhibiting (MAOI) activity. Psychotria viridis contains the 5HT2A/2C/1A receptor agonist hallucinogen N,N-dimethyltryptamine (DMT). Usual desired effects include hallucination, dissociation, mood alteration and perception change. Undesired findings previously reported are nausea, vomiting, hypertension, and tachycardia. Methods All human exposure calls reported to the American Association of Poison Controls Centers' (AAPCC) National Poison Data System (NPDS) between September 1, 2005 and September 1, 2015 were reviewed. Cases were filtered for specific Plant derived ayahuasca-related product codes. Abstracted data included the following: case age and gender, exposure reason, exposure route, clinical manifestations, treatments given, medical outcomes and fatality. Results Five hundred and thirty-eight exposures to ayahuasca botanical products were reported. The majority of the calls to poison control centers came from healthcare facilities (83%). The most common route of exposure was ingestion. Most cases were men (437, 81%, 95% CI 77.7% - 84.3%). The median age was 21 (IQR 18-29). Most exposures were acute. Three hundred thirty-seven (63%) were reported to have a major or moderate clinical effect. The most common clinical manifestations reported were hallucinations (35%), tachycardia (34%), agitation (34%), hypertension (16%), mydriasis (13%) and vomiting (6%). Benzodiazepines were commonly given (30%). There were 28 cases in the series who required endotracheal intubation (5%). Four cases were reported to have had a cardiac arrest and 7 a respiratory arrest. Twelve cases had a seizure. Reports of exposures called to poison centers appeared to increase during this period based on annual estimates. Three fatalities were reported. Conclusions Ayahuasca use appears to be rising in the United States based on calls to poison control centers. While most use is reported to be safe and well tolerated, with possible beneficial effects, serious and life threatening adverse manifestations are possible. Most of the exposures reported to poison control centers were young people, more likely to be men and already in a healthcare facility. Further research, which includes comprehensive drug testing, will be needed to better identify the risks and effects of ayahuasca use.
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Ayahuasca exposure: descriptive analysis of calls to US poison control centers from 2005 to 2015
Journal of Medical Toxicology, 2016Co-Authors: C. William Heise, Daniel E. BrooksAbstract:Background Ayahuasca is a Hallucinogenic Plant preparation which usually contains the vine Banisteriopsis caapi and the shrub Psychotria viridis. This tea originates from the Amazon Basin where it is used in religious ceremonies. Because interest in these religious groups spreading as well as awareness of use of ayahuasca for therapeutic and recreational purposes, its use is increasing. Banisteriopsis caapi is rich in β-carbolines, especially harmine, tetrahydroharmine and harmaline, which have monoamine oxidase inhibiting (MAOI) activity. Psychotria viridis contains the 5HT2A/2C/1A receptor agonist hallucinogen N,N-dimethyltryptamine (DMT). Usual desired effects include hallucination, dissociation, mood alteration and perception change. Undesired findings previously reported are nausea, vomiting, hypertension, and tachycardia.
