Synthetic Amphetamine Derivatives

Lapoint, Jeff; Dargan, Paul I.; Hoffman, Robert S.

doi:10.1016/b978-0-12-415816-0.00007-9

Cited by 7 publications

(5 citation statements)

References 57 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…2,5-Dimethoxy-4-iodoamphetamine (DOI) is a substituted amphetamine but is not a stimulant. It is a potent 5-HT 2 A serotonin receptor agonist and is used recreationally as a hallucinogenic drug ( Lapoint et al, 2013 ). DOI induces cutaneous vascular constriction in rabbits and rats, and this is the suggested cause of hyperthermia resulting from serotonin receptor stimulation ( Blessing and Seaman, 2003 ).…”

Section: Lsec and Drug Interactionsmentioning

confidence: 99%

The wHole Story About Fenestrations in LSEC

et al. 2021

View full text Add to dashboard Cite

The porosity of liver sinusoidal endothelial cells (LSEC) ensures bidirectional passive transport of lipoproteins, drugs and solutes between the liver capillaries and the liver parenchyma. This porosity is realized via fenestrations – transcellular pores with diameters in the range of 50–300 nm – typically grouped together in sieve plates. Aging and several liver disorders severely reduce LSEC porosity, decreasing their filtration properties. Over the years, a variety of drugs, stimulants, and toxins have been investigated in the context of altered diameter or frequency of fenestrations. In fact, any change in the porosity, connected with the change in number and/or size of fenestrations is reflected in the overall liver-vascular system crosstalk. Recently, several commonly used medicines have been proposed to have a beneficial effect on LSEC re-fenestration in aging. These findings may be important for the aging populations of the world. In this review we collate the literature on medicines, recreational drugs, hormones and laboratory tools (including toxins) where the effect LSEC morphology was quantitatively analyzed. Moreover, different experimental models of liver pathology are discussed in the context of fenestrations. The second part of this review covers the cellular mechanisms of action to enable physicians and researchers to predict the effect of newly developed drugs on LSEC porosity. To achieve this, we discuss four existing hypotheses of regulation of fenestrations. Finally, we provide a summary of the cellular mechanisms which are demonstrated to tune the porosity of LSEC.

show abstract

Section: Lsec and Drug Interactionsmentioning

confidence: 99%

The wHole Story About Fenestrations in LSEC

et al. 2021

View full text Add to dashboard Cite

show abstract

“…(Rahman, Fazilah, & Effarizah, 2015), elemicin in food upto 0.05 mg/kg (De Vincenzi, De Vincenzi, & Silano, 2004) and 0.02–1.88 mg/L of DMT, 5‐MeO‐DMT, harmaline, tetrahydroharmine, harmine in cardiac blood (Sklerov, Levine, Moore, King, & Fowler, 2005). Myristicin of nutmeg oil is metabolized to the controlled drugs namely, MMDA, MDMA, MMDMA (Clark, DeRuiter, & Noggle, 1996), safrole to MDA (Shulgin, Sargent, & Naranjo, 1967), elemicin to 3,4,5‐Trimethoxyamphetamine (Lapoint, Dargan, & Hoffman, 2013), whereas 5‐MeO‐DMT, DMT were used as controlled substances in USA and UK (Federal Register, 2010; Tittarelli, Mannocchi, Pantano, & Saverio Romolo, 2015; Waller & Sampson, 2018).…”

Section: Poisoning and Toxicitymentioning

confidence: 99%

Nutmegs and wild nutmegs: An update on ethnomedicines, phytochemicals, pharmacology, and toxicity of the Myristicaceae species

Barman

Bora

Saikia

et al. 2021

Phytotherapy Research

View full text Add to dashboard Cite

Prized medicinal spice true nutmeg is obtained from Myristica fragrans Houtt. Rest species of the family Myristicaceae are known as wild nutmegs. Nutmegs and wild nutmegs are a rich reservoir of bioactive molecules and used in traditional medicines of Europe, Asia, Africa, America against madness, convulsion, cancer, skin infection, malaria, diarrhea, rheumatism, asthma, cough, cold, as stimulant, tonics, and psychotomimetic agents. Nutmegs are cultivated around the tropics for high‐value commercial spice, used in global cuisine. A thorough literature survey of peer‐reviewed publications, scientific online databases, authentic webpages, and regulatory guidelines found major phytochemicals namely, terpenes, fatty acids, phenylpropanoids, alkanes, lignans, flavonoids, coumarins, and indole alkaloids. Scientific names, synonyms were verified with http://www.theplantlist.org. Pharmacological evaluation of extracts and isolated biomarkers showed cholinesterase inhibitory, anxiolytic, neuroprotective, anti‐inflammatory, immunomodulatory, antinociceptive, anticancer, antimicrobial, antiprotozoal, antidiabetic, antidiarrhoeal activities, and toxicity through in‐vitro, in‐vivo studies. Human clinical trials were very few. Most of the pharmacological studies were not conducted as per current guidelines of natural products to ensure repeatability, safety, and translational use in human therapeutics. Rigorous pharmacological evaluation and randomized double‐blind clinical trials are recommended to analyze the efficacy and therapeutic potential of nutmeg and wild nutmegs in anxiety, Alzheimer's disease, autism, schizophrenia, stroke, cancer, and others.

show abstract

“…Thus, one may assume that the cases of severe toxicity reported after recreational use of these drugs (e.g. Elliott, 2000;De Letter et al, 2001;Martin, 2001;Lamberth et al, 2008), which resemble "serotonin syndrome" symptoms (Lapoint et al, 2013), are related to a sustained increase of synaptic 5-HT and DA resulting from both monoamine reverse transport and MAO-A inhibition. Furthermore, as many AMPH derivatives are monoamine transporter substrates (Simmler et al, 2013;Sitte and Freissmuth, 2015), even in those cases in which relatively weak MAOI activity is demonstrated, these drugs might be concentrated in presynaptic nerve terminals or glial cells, and some enzyme inhibition could occur (Heal et al, 2013).…”

Section: Summary Of Structure-activity Relationships and Implicationsmentioning

confidence: 99%

Amphetamine Derivatives as Monoamine Oxidase Inhibitors

2020

View full text Add to dashboard Cite

Amphetamine and its derivatives exhibit a wide range of pharmacological activities, including psychostimulant, hallucinogenic, entactogenic, anorectic, or antidepressant effects. The mechanisms of action underlying these effects are usually related to the ability of the different amphetamines to interact with diverse monoamine transporters or receptors. Moreover, many of these compounds are also potent and selective monoamine oxidase inhibitors. In the present work, we review how structural modifications on the aromatic ring, the amino group and/or the aliphatic side chain of the parent scaffold, modulate the enzyme inhibitory properties of hundreds of amphetamine derivatives. Furthermore, we discuss how monoamine oxidase inhibition might influence the pharmacology of these compounds.

show abstract

Synthetic Amphetamine Derivatives

Cited by 7 publications

References 57 publications

The wHole Story About Fenestrations in LSEC

The wHole Story About Fenestrations in LSEC

Nutmegs and wild nutmegs: An update on ethnomedicines, phytochemicals, pharmacology, and toxicity of the Myristicaceae species

Amphetamine Derivatives as Monoamine Oxidase Inhibitors

Contact Info

Product

Resources

About