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All 2 posts Subject: DE Nichols: Amphetamine Designer Drugs Please login to post Down

Rhodium
(Chief Bee)
06-06-04 21:44
No 511835
User Picture       DE Nichols: Amphetamine Designer Drugs
(Rated as: excellent)

Substituted Amphetamine Controlled Substance Analogues
David E. Nichols
Cocaine, Marijuana, Designer Drugs: Chemistry, Pharmacology, and Behavior: Chapter 14, pp. 175-186 (https://www.rhodium.ws/chemistry/designer.drugs.nichols.html)
^{Editors: Kinfe K. Redda, Charles A. Walker, Gene Barnett, 1989 CRC Press, Inc. Boca Raton, FL}

Introduction

First and foremost, drug abuse is a social problem rather than a physiological one. It is not entirely clear that any solutions can be found by focusing attention on the drugs themselves, rather than on the societal conditions that lead to drug abuse. Therefore, it seems appropriate to consider some of the broader issues, rather than to deal exclusively with the chemistry or structure-activity relationships of hallucinogenic amphetamine derivatives.

The task is made doubly difficult by this author's belief that although controlled substance analogues of the hallucinogenic amphetamine type possess the potential for nearly unimaginable tragedy, at the same time, research with these substances holds hope for future advances in psychiatric medicine.

On the one hand, if hallucinogenic drugs can be seen as useful substances, they may serve as a potentially rich source of new psychotherapeutic compounds, which could catalyze a revolution in psychiatry and psychotherapy. However, virtually no approved clinical research is being carried out with hallucinogens, and this appears to be a continuing situation in the foreseeable future. And, while there may be no clinical research, "recreational" use of hallucinogenic controlled substance analogues continues pretty much unabated.

^{The Hive - Clandestine Chemists Without Borders}

Rhodium
(Chief Bee)
10-21-04 15:05
No 536968
User Picture       Designer Drugs: An Overview (Chapter 13)

Designer Drugs: An Overview
Gene Barnett & Rao S. Rapaka
Cocaine, Marijuana, Designer Drugs: Chemistry, Pharmacology, and Behavior: Chapter 13, pp. 163-174 (https://www.rhodium.ws/chemistry/designer.drugs.overview.html)
^{Editors: Kinfe K. Redda, Charles A. Walker, Gene Barnett, 1989 CRC Press, Inc. Boca Raton, FL}

Introduction"Designer drugs are analogs, or chemical cousins, of controlled substances that
are designed to produce effects similar to the controlled substances they mimick.
By slightly altering the chemical formula of a controlled substance ...
a new drug is created which will produce the high or euphoria the user wants."
This definition was given during Congressional hearings on designer drugs in 1985 where the illicit drug trade was estimated to be a $110 billion per year industry in the U.S., which is about three times the total sales of the U.S. pharmaceutical industry. The illicit importation was an estimated 10 tons of heroin, 85 tons of cocaine, and 15,000 tons of marijuana. Further, "The production of illicit drugs abroad continues unabated, and in our own country illicit marijuana has become a major cash crop." The designer drug portion of the illicit market is estimated at $1 billion and primarily in opiate-type and phenylisopropylamine-type street drugs at the current time.

Why is there drug abuse? Why do people consume designer drugs or other illicit drugs? The answer commonly given: because it feels good. The drugs that are so used are psy choactive drugs, ones that produce effects on thought, feeling, mood, self-perception, and give a sense of "high" or intoxication. Self-administration of drugs for nonmedical, indeed, recreational purposes can be a hazard as it may lead to compulsive or addictive use. Drugs from the illicit marketplace have the additional hazard of containing impurities or untested chemicals that can be toxic and life threatening. Efforts to understand why opiates and hallucinogens are self-administered yields the following descriptions. Intravenous use of an opiate produces warm flushing of the skin and sensations in the lower abdomen described by addicts as similar in intensity and quality to sexual orgasm. Consumption of a hallucinogen drug, or other central nervous system sympathomimetic drugs, such as cocaine, produces a heightened awareness of sensory input, often with an enhanced sense of clarity, and the user receives vivid and unusual sensory experiences, attention is focused inward with a sense of union with the cosmos or mankind. The phenomenon of drug abuse has become a sophis ticated and relatively new area of study of the human being from perspectives of physiology and psychology, where concern is given to such issues as tolerance and cross tolerance, dependence and addiction, and induced behavioral reinforcement that will certainly lead to a better understanding of the human organism.

The design of new drugs often utilizes basic principles of the chemistry laboratory whereby the structure of a drug molecule is slightly altered in order to alter the pharmacological activity. This principle of structure-activity relationships, known as SAR, has been applied to many medically approved drugs that are in the marketplace. For the opiates, SAR studies have been pursued in the search for a nonaddicting analgesic for the treatment of pain. Slight structural changes have produced new drugs with altered receptor-binding properties and altered potency or activity. Basic research on the opiates during the last decade has lead to important scientific discoveries of multiple opiate receptors, the endogenous opioids, and renewed interest in the structure and function of polypeptides. The hallucinogen family of drugs are not as well understood as the opiates. A 1978 conference on quantitative SAR studies of the opiates and hallucinogens found detailed discussions on opiate receptor binding and sophisticated arguments as to the existence of multiple opioid receptors with different pharmacologic properties, while discussions on the hallucinogens were in a relatively early stage of development. There are substantial benefits to be gained from a basic understanding of how drugs of this family, many of which can be classified as sympathomimetic drugs together with cocaine, interact and/or interfere with the chemical messengers or neurotransmitters of the autonomic nervous system.

Clandestine production of drugs, so called street drugs, is intended to avoid federal regulation and control. The result is availability of unknown substances of unknown purity that may have the potential to cause serious toxicity with potentially dangerous health consequences for the naive drug user. A review of illicit drugs and analogues produced by the clandestine pharmaceutical industry concludes that the quality of personnel involved in drug synthesis ranges from cookbook amateurs to highly skilled chemists. And quite surprisingly, "most of these new analogs have been previously reported in the literature with animal data that suggest they would be reasonably active and have similar pharmacological effects to the lead compound in the series".

^{The Hive - Clandestine Chemists Without Borders}

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	All 2 posts		Subject: DE Nichols: Amphetamine Designer Drugs		Please login to post		Down


		Rhodium (Chief Bee) 06-06-04 21:44 No 511835				DE Nichols: Amphetamine Designer Drugs (Rated as: excellent)
						Substituted Amphetamine Controlled Substance Analogues David E. Nichols Cocaine, Marijuana, Designer Drugs: Chemistry, Pharmacology, and Behavior: Chapter 14, pp. 175-186 (https://www.rhodium.ws/chemistry/designer.drugs.nichols.html) ^{Editors: Kinfe K. Redda, Charles A. Walker, Gene Barnett, 1989 CRC Press, Inc. Boca Raton, FL} Introduction First and foremost, drug abuse is a social problem rather than a physiological one. It is not entirely clear that any solutions can be found by focusing attention on the drugs themselves, rather than on the societal conditions that lead to drug abuse. Therefore, it seems appropriate to consider some of the broader issues, rather than to deal exclusively with the chemistry or structure-activity relationships of hallucinogenic amphetamine derivatives. The task is made doubly difficult by this author's belief that although controlled substance analogues of the hallucinogenic amphetamine type possess the potential for nearly unimaginable tragedy, at the same time, research with these substances holds hope for future advances in psychiatric medicine. On the one hand, if hallucinogenic drugs can be seen as useful substances, they may serve as a potentially rich source of new psychotherapeutic compounds, which could catalyze a revolution in psychiatry and psychotherapy. However, virtually no approved clinical research is being carried out with hallucinogens, and this appears to be a continuing situation in the foreseeable future. And, while there may be no clinical research, "recreational" use of hallucinogenic controlled substance analogues continues pretty much unabated. ^{The Hive - Clandestine Chemists Without Borders}



		Rhodium (Chief Bee) 10-21-04 15:05 No 536968				Designer Drugs: An Overview (Chapter 13)
						Designer Drugs: An Overview Gene Barnett & Rao S. Rapaka Cocaine, Marijuana, Designer Drugs: Chemistry, Pharmacology, and Behavior: Chapter 13, pp. 163-174 (https://www.rhodium.ws/chemistry/designer.drugs.overview.html) ^{Editors: Kinfe K. Redda, Charles A. Walker, Gene Barnett, 1989 CRC Press, Inc. Boca Raton, FL} Introduction"Designer drugs are analogs, or chemical cousins, of controlled substances that are designed to produce effects similar to the controlled substances they mimick. By slightly altering the chemical formula of a controlled substance ... a new drug is created which will produce the high or euphoria the user wants." This definition was given during Congressional hearings on designer drugs in 1985 where the illicit drug trade was estimated to be a $110 billion per year industry in the U.S., which is about three times the total sales of the U.S. pharmaceutical industry. The illicit importation was an estimated 10 tons of heroin, 85 tons of cocaine, and 15,000 tons of marijuana. Further, "The production of illicit drugs abroad continues unabated, and in our own country illicit marijuana has become a major cash crop." The designer drug portion of the illicit market is estimated at $1 billion and primarily in opiate-type and phenylisopropylamine-type street drugs at the current time. Why is there drug abuse? Why do people consume designer drugs or other illicit drugs? The answer commonly given: because it feels good. The drugs that are so used are psy choactive drugs, ones that produce effects on thought, feeling, mood, self-perception, and give a sense of "high" or intoxication. Self-administration of drugs for nonmedical, indeed, recreational purposes can be a hazard as it may lead to compulsive or addictive use. Drugs from the illicit marketplace have the additional hazard of containing impurities or untested chemicals that can be toxic and life threatening. Efforts to understand why opiates and hallucinogens are self-administered yields the following descriptions. Intravenous use of an opiate produces warm flushing of the skin and sensations in the lower abdomen described by addicts as similar in intensity and quality to sexual orgasm. Consumption of a hallucinogen drug, or other central nervous system sympathomimetic drugs, such as cocaine, produces a heightened awareness of sensory input, often with an enhanced sense of clarity, and the user receives vivid and unusual sensory experiences, attention is focused inward with a sense of union with the cosmos or mankind. The phenomenon of drug abuse has become a sophis ticated and relatively new area of study of the human being from perspectives of physiology and psychology, where concern is given to such issues as tolerance and cross tolerance, dependence and addiction, and induced behavioral reinforcement that will certainly lead to a better understanding of the human organism. The design of new drugs often utilizes basic principles of the chemistry laboratory whereby the structure of a drug molecule is slightly altered in order to alter the pharmacological activity. This principle of structure-activity relationships, known as SAR, has been applied to many medically approved drugs that are in the marketplace. For the opiates, SAR studies have been pursued in the search for a nonaddicting analgesic for the treatment of pain. Slight structural changes have produced new drugs with altered receptor-binding properties and altered potency or activity. Basic research on the opiates during the last decade has lead to important scientific discoveries of multiple opiate receptors, the endogenous opioids, and renewed interest in the structure and function of polypeptides. The hallucinogen family of drugs are not as well understood as the opiates. A 1978 conference on quantitative SAR studies of the opiates and hallucinogens found detailed discussions on opiate receptor binding and sophisticated arguments as to the existence of multiple opioid receptors with different pharmacologic properties, while discussions on the hallucinogens were in a relatively early stage of development. There are substantial benefits to be gained from a basic understanding of how drugs of this family, many of which can be classified as sympathomimetic drugs together with cocaine, interact and/or interfere with the chemical messengers or neurotransmitters of the autonomic nervous system. Clandestine production of drugs, so called street drugs, is intended to avoid federal regulation and control. The result is availability of unknown substances of unknown purity that may have the potential to cause serious toxicity with potentially dangerous health consequences for the naive drug user. A review of illicit drugs and analogues produced by the clandestine pharmaceutical industry concludes that the quality of personnel involved in drug synthesis ranges from cookbook amateurs to highly skilled chemists. And quite surprisingly, "most of these new analogs have been previously reported in the literature with animal data that suggest they would be reasonably active and have similar pharmacological effects to the lead compound in the series". ^{The Hive - Clandestine Chemists Without Borders}

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