Normethadone is a derivate of opioid analgetic methadone, used as component of antitussive drops in Canada. Illicit drug.

Levlofexidine is R-enantiomer of a α2A adrenergic receptor agonist Lofexidine. Levlofexidine (as a component of Lofexidine) can be used as a short-acting anti-hypertensive but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. Lofexidine is approved in the United Kingdom but is still undergoing clinical trials in the United States. Levlofexidine showed an approximately 9-fold higher affinity than Dexlofexidine for the alpha 2-adrenoceptor-like binding sites in rat brain membranes identified by [3H]-clonidine and was 4 times more potent at displacing [3H]-prazosin from alpha 1-adrenoceptors. The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated and has not yet been shown to be an effective treatment.

Levopropylhexedrine acts similar to amphetamine, at therapeutic doses has anorexigenic effect.

Pholcodine is an opioid that has been widely used worldwide since 1950 for the treatment of non-productive cough in children and adults. Illicit drug. Additionally Pholcodine is a marker for sensitization to neuromuscular blocking agents (NMBA) and is intended for use as a diagnostic tool in NMBA-induced anaphylaxis.

Tiratricol (also known as TRIAC or triiodothyroacetic acid) is a thyroid hormone analogue, which has been studied since the 1950s. Tiratricol is used as a dietary supplement for thyroid problems including thyroid cancer. It is also used for increasing metabolic rate for weight loss, and reducing cellulite. In the US, the Food and Drug Administration (FDA) has determined that the product Triax (TRIAC, tiratricol) is not a dietary supplement but an unapproved new drug containing a powerful thyroid hormone, which may cause serious health consequences. The State of Missouri embargoed the product at its distributor (Syntrax) and the Utah-based manufacturer (Pharmatech) has agreed to stop distributing any product containing the ingredient TRIAC. The FDA has issued recalls for other tiratricol-containing products, including Tricana Metabolic Hormone Analogue, Tria-Cutz Thyroid Stimulator Dietary Supplement Capsules, and Sci-Fi-Tri-Cuts Dietary Supplement Capsules. Tiratricol is a prescription drug in France used for therapy of thyroid hormone resistance and therapy of thyroid cancer.

Pholcodine is an opioid that has been widely used worldwide since 1950 for the treatment of non-productive cough in children and adults. Illicit drug. Additionally Pholcodine is a marker for sensitization to neuromuscular blocking agents (NMBA) and is intended for use as a diagnostic tool in NMBA-induced anaphylaxis.

Fenethylline (generic name Captagon) is a codrug of amphetamine and theophylline. In the fenetylline molecule, theophylline is covalently linked with amphetamine via an alkyl chain. It was formerly used to treat conditions such as ADHD, narcolepsy, and depression, but its use has been banned because of the potential for abuse. Amphetamine, an agonist for trace amine-associated receptor 1 (TAAR1) with enhancing dopamine signaling (an increase of irritability, aggression, etc.), is the main cause of Captagon addiction. Theophylline, an antagonist that blocks adenosine receptors (e.g. A2aR) in the brain responsible for restlessness and painlessness, may attenuate the behavioral sensitization caused by amphetamine. Fenethylline is included in a list of compounds to be considered by a World Health Organization (WHO) Expert Committee in April 1985 for possible international scheduling under the Convention on Psychotropic Substances, 1971. Fenethylline re-emerged because of its widespread abuse by Middle Eastern young adults. Terrorist groups such as the Islamic State to enhance what they consider desirable characteristics - aggressiveness, alertness, and fearlessness - in their recruits, promote it.

Fenethylline (generic name Captagon) is a codrug of amphetamine and theophylline. In the fenetylline molecule, theophylline is covalently linked with amphetamine via an alkyl chain. It was formerly used to treat conditions such as ADHD, narcolepsy, and depression, but its use has been banned because of the potential for abuse. Amphetamine, an agonist for trace amine-associated receptor 1 (TAAR1) with enhancing dopamine signaling (an increase of irritability, aggression, etc.), is the main cause of Captagon addiction. Theophylline, an antagonist that blocks adenosine receptors (e.g. A2aR) in the brain responsible for restlessness and painlessness, may attenuate the behavioral sensitization caused by amphetamine. Fenethylline is included in a list of compounds to be considered by a World Health Organization (WHO) Expert Committee in April 1985 for possible international scheduling under the Convention on Psychotropic Substances, 1971. Fenethylline re-emerged because of its widespread abuse by Middle Eastern young adults. Terrorist groups such as the Islamic State to enhance what they consider desirable characteristics - aggressiveness, alertness, and fearlessness - in their recruits, promote it.

Fenethylline (generic name Captagon) is a codrug of amphetamine and theophylline. In the fenetylline molecule, theophylline is covalently linked with amphetamine via an alkyl chain. It was formerly used to treat conditions such as ADHD, narcolepsy, and depression, but its use has been banned because of the potential for abuse. Amphetamine, an agonist for trace amine-associated receptor 1 (TAAR1) with enhancing dopamine signaling (an increase of irritability, aggression, etc.), is the main cause of Captagon addiction. Theophylline, an antagonist that blocks adenosine receptors (e.g. A2aR) in the brain responsible for restlessness and painlessness, may attenuate the behavioral sensitization caused by amphetamine. Fenethylline is included in a list of compounds to be considered by a World Health Organization (WHO) Expert Committee in April 1985 for possible international scheduling under the Convention on Psychotropic Substances, 1971. Fenethylline re-emerged because of its widespread abuse by Middle Eastern young adults. Terrorist groups such as the Islamic State to enhance what they consider desirable characteristics - aggressiveness, alertness, and fearlessness - in their recruits, promote it.

Higenamine HCl (norcoclaurine) is a plant-based alkaloid widely used as nutritional supplement in food and beverage industries. It exists in variety of plants including Tinospora crispa, Nandina domestica, Gnetum Parvifolium C.Y. Cheng, sarum Heterotropoides, Nelumbo nucifera. It was initially isolated from Aconitum and identified as the active cardiotonic component of this medicinal plant used as local and traditional medicines in many Asian regions for the treatment of various diseases such as collapse, syncope, painful joints, oedema, bronchial asthma etc. Various pharmacological properties and potentially multi-spectral medical applications of higenamine have been reviled in many in vitro and in vivo studies conducted in animals and humans. Pharmacological properties of higenamine include positive inotropic and chronotropic effect, activating slow channel effect, vascular and tracheal relaxation effect, anti-thrombotic, anti-apoptotic and anti-oxidative effect, anti-inflammatory and immunomodulatory effect. Studies on higenamine showed potential therapeutic effects for diseases like heart failure, disseminated intravascular coagulation (DIC), shock, arthritis, asthma, ischemia/reperfusion injuries and erectile dysfunction. Higenamine has been tested as a candidate of pharmacologic stress agent in the detection of coronary artery diseases (CADs) in human clinical studies in China. In animal models, higenamine has been demonstrated to be a β2 adrenoreceptor agonist. It partly exerts its actions by the activation of adenylate cyclase, responsible for boosting the cellular concentrations of the adrenergic second messenger, cAMP. Via a beta-adrenoceptor mechanism higenamine, induced relaxation in rat corpus cavernosum, leading to improved vasodilation and erectile function. Related to improved vasodilatory signals, higenamine has been shown to possess antiplatelet and antithrombotic activity via a cAMP-dependent pathway, suggesting it may contribute to enhanced vasodilation and arterial integrity. Anti-apoptotic and cardiac protective effects of higenamine were shown to be mediated by the β2-AR/PI3K/AKT cascade. Higenamine is marketed as a dietary supplement for weight loss and sport performance, and is added to many fat burning supplements. Along with many other β2 agonists, higenamine is prohibited by World Anti-Doping Agency for use in sports.