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CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its...
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Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

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Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
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CNS Stimulants: Psychedelic Agents01:22

CNS Stimulants: Psychedelic Agents

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Hallucinogens, also known as psychedelic drugs, are a class of substances known for their ability to alter perception, cognition, and emotions. Despite their profound effects on the mind, these drugs are non-addictive, setting them apart from many other abused substances. The mechanism of action of these drugs lies in their impact on the 5-HT2A receptor in the brain. Upon activation, this receptor couples to Gq-type G proteins, triggering a cascade that releases intracellular calcium. This...
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Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

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Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
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Hallucinogens and Psychedelics01:27

Hallucinogens and Psychedelics

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Hallucinogens are psychoactive substances that profoundly alter perceptual experiences, generating unreal visual and sensory images. Often referred to as psychedelic drugs — a term derived from the Greek words "psyche" (mind) and "delos" (revealing) — these substances include marijuana and lysergic acid diethylamide (LSD), among others. These drugs vary in intensity and effects.
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An Overview of Psychoactive Drugs01:28

An Overview of Psychoactive Drugs

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Psychoactive drugs impact brain function, influencing perception, mood, consciousness, cognition, and behavior. These substances are grouped based on their effects and the mechanisms by which they act.
Stimulants such as cocaine, amphetamines, and nicotine enhance brain activity, leading to increased alertness, attention, and energy. These drugs typically raise heart rate, blood pressure, and body temperature. While they can induce feelings of euphoria, their misuse can result in severe health...
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Related Experiment Video

Updated: Dec 27, 2025

Author Spotlight: An Efficient Methodology to Confidently Differentiate and Characterize Fentanyl Analogs
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Author Spotlight: An Efficient Methodology to Confidently Differentiate and Characterize Fentanyl Analogs

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Nonpsychotropic synthetic cannabinoids.

E Pop1

  • 1Alchem Laboratories Corporation, 13305 Rachael Boulevard, Alachua, FL, USA. emilpop@aol.com

Current Pharmaceutical Design
|July 21, 2000
PubMed
Summary

Synthetic dexanabinol (HU-211) derivatives, unlike natural cannabinoids, lack receptor affinity but show neuroprotection. Novel 6aS-trans cannabinoids were synthesized, including water-soluble options, for therapeutic development.

Area of Science:

  • Medicinal Chemistry
  • Neuropharmacology
  • Synthetic Organic Chemistry

Background:

  • Natural cannabinoids interact with cannabinoid receptors, mediating various physiological effects.
  • Synthetic dexanabinol (HU-211), a 6aS-trans enantiomer, lacks cannabinoid receptor affinity and cannabimimetic activity.
  • Dexanabinol exhibits significant neuroprotective properties, indicating therapeutic potential.

Purpose of the Study:

  • To synthesize and characterize novel 6aS-trans cannabinoid derivatives.
  • To explore water-soluble derivatives and congeners of dexanabinol.
  • To extend the series of synthetic cannabinoids with potential therapeutic applications.

Main Methods:

  • Enantioselective synthesis of 6aS-trans cannabinoids.
  • Characterization of novel synthetic compounds.

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  • Evaluation of physicochemical properties, including water solubility.
  • Main Results:

    • A series of novel 6aS-trans cannabinoid derivatives were successfully synthesized.
    • Water-soluble derivatives and dexanabinol congeners were obtained.
    • The synthetic compounds expand the chemical space for exploring neuroprotective agents.

    Conclusions:

    • The synthesized 6aS-trans cannabinoids represent novel chemical entities.
    • These compounds offer potential for developing new therapeutic agents, particularly for neuroprotection.
    • The development of water-soluble derivatives may improve drug delivery and therapeutic efficacy.