Synthetic cannabinoid Receptor Agonists
Synthetic cannabinoid Receptor Agonists
Synthetic cannabinoid Receptor Agonists are also known as spice. These are a collection of herbs or plant material which has been sprayed with synthetic cannabinoid receptor agonists, often referred to as synthetic cannabinoids, producing a cannabis-like effect when smoked. Today there are more than one type of cannabinoids that have been identified but they are all active as they mimic the psychoactive effects of THC (tetrahydrocannabinol), the active principle in cannabis. Most compounds come from the JWH chemical family, such as JWH-018.
For emphasis it is good to repeat that these synthetic cannabinoids are functionally similar to tetrahydrocannabinol often shortened as THC. THC is the most active principle of cannabis. Like THC, they bind to the same cannabinoid receptors in the brain and other organs as the endogenous ligand anandamide. More correctly designated as cannabinoid receptor agonists, they were initially developed over the past forty years as therapeutic agents, often for the treatment of pain. However, it proved difficult to separate the desired properties from unwanted psychoactive effects.

In the past years especially in the late 2008, several cannabinoids were detected in herbal smoking mixtures and incense as well as room odorisers. Typical of these were Spice Gold, Spice Silver and Yucatan Fire, but many other products later appeared. They do not contain tobacco or cannabis but when smoked, produce effects similar to those of cannabis. These products are typically sold via the Internet and in ‘head shops’. The spices are therefore as dangerous as cannabis and so should be avoided.
The fact that these spices are referred to as synthetic cannabinoids does not mean that they are similar to the real cannabinoids in all aspects in fact most of these synthetic cannabinoids are not related to the real cannabinoids in structure and hence though they can mimic the activities of the cannabinoids but they may work in a way that will cause more harm. The cannabinoid receptor agonists form a diverse group, but most are lipid soluble and non-polar, and consist of 22 to 26 carbon atoms. This therefore means that they would therefore volatilize readily when smoked. A common structural feature is a side-chain, where optimal activity requires more than four and up to nine saturated carbon atoms. The synthetic cannabinoids can be classified into seven major structural groups. These groups are;
- Naphthoylindoles (e.g. JWH-018, JWH-073 and JWH-398).
- Phenylacetylindoles (i.e. benzoylindoles, e.g. JWH-250).
- Cyclohexylphenols (e.g. CP 47,497 and homologues of CP 47,497).
- Classical cannabinoids (e.g. HU-210).
Other cannabinoid receptor agonists include substances such as oleamide. Oleamide is an endogenous substance that is also used in plastics manufacture. Another one is methanandamide. Oleamide and methanandamide are both related to anandamide in structure. Despite the similarities in structure with the anandamide the activities of these two synthetic cannabinoids have been questioned. It is thought that neither methanandamide nor other arachidonyl derivatives related to anandamide would be sufficiently volatile to be smoked. Certain fluorosulfonates exhibit agonist activity at cannabinoid receptors, as does naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone, but the latter appears not to be psychoactive, at least when administered orally.
Physical state
Most of these synthetic cannabinoids are either solids or oils as they exist in pure state. Smoking mixtures are usually sold in metal-foil sachets, typically containing 3 g of dried vegetable matter to which one or more of the cannabinoids have been added. Typically, a solution of the cannabinoids has been sprayed onto the herbal mixture to give it the drug effect. Just like any other business oriented producer you will find a number of plants listed on the packaging but the plants mentioned on the packaging may not even be present. This is utmost dangerous as you may be using these spices thinking you are safe based on the ingredients wrote on the packaging while in real sense you are using substances you do not even know. These spices are often sold while containing high amounts of Vitamin E which is purported to be used in masking the analysis of the most active cannabinoids. The producers of these spices will put more cannabinoids in the samples to confound the forensic chemical detection.
The cannabinoid receptor agonists mimic the effects of THC and anandamide by interacting with the CB1 receptor in the brain. Several research studies have shown that some synthetic compounds bind more strongly to this receptor than THC as measured by the affinity constant Ki. All of the cannabinoids found in smoking mixtures have, like THC (Ki = 10.2nM), high affinity to the CB1receptor although small variations in Ki values occur between different publications. The substance HU-210 has a particularly low value of Ki (0.06nM), and it binds over 100 times more tightly to the CB1 receptor than THC.
However, little is known about the detailed pharmacology and toxicology of the synthetic cannabinoids and few formal human studies have been published. It is possible that, apart from high potency, some cannabinoids could have particularly long half-lives potentially leading to a prolonged psychoactive effect. In addition, there could be considerable inter-and intra-batch variability in smoking mixtures, both in terms of substances present and their quantity. Thus, there is a higher potential for overdose than with cannabis.
Finally, Dr. Dalal Akoury (MD) is an experienced doctor who has been in the frontline fighting drug addiction. He runs a website that equips readers of better ways to overcome not only drug addiction but also serious health problems that have caused nightmares to the world population. Get in touch with her today and learn more.
Synthetic cannabinoid Receptor Agonists







The greatest challenge for physicians today is to be up to par with the new and remerging drugs of abuse. The problem is the law enforcers have declared certain drugs that were perceived to have medicinal qualities into illegal drugs. Most of these drugs are those used in cooling pain. Having these drugs classified as illegal has led to many street doctors to adopt ways through which they can continue using such drugs without being at loggerheads with the law enforcers and that has led to mixing certain substances with these drugs in a bid to conceal what the real contents of the drugs are. They have also branded this drugs with strange names all in a in a bid to hide them from the law enforcers. The packages of these drugs are written as ‘not for human consumption’ among other strange names that has been given to these new and re-emerging drugs of abuse to enable them trade safe. Emerging drugs of abuse are forever changing and involve manipulation of basic chemical structures to avoid legal ramifications. The structural changes are important to those dealing in these drugs as they help them evade forensic chemical tests hurdles. The names given to these drugs may not even have a relation to their contents and so not as important as understanding the classes of these drugs. Most of the synthetic new drugs of abuse result in psychoactive and sympathomimetic effects.






Any drug when taken for non-medical purposes then it is termed abused. Today there are very many drugs that are being used for sheer feeling of euphoria the users derive from them. These drugs are common in streets needless to mention some of the drugs that are used in hospitals for medicinal purposes have also been abused greatly. When a particular drug is used for quite a long time for non-medical purpose it becomes very toxic to the body. Substance abuse is a vice that needs to be fought at all costs and from all fronts as it has opened avenues through which lives have been lost. The problems that a person can suffer from long-term drug abuse spring from all the dimensions of a person’s health be it psychological health, mental health, physical health as well as his social relations. A person who is a victim to drug abuse may fail to cater for family needs, school obligations and even fail to have peace within him as he will be having lots of personal and interpersonal conflicts. Drug and substance dependence is commonly known as addiction. Drug or substance dependence is characterized by change in behaviors of a person. Most common behavior being the need to use more quantities of the substance. When a person is dependent on a given substance his life begins to revolve around it and it seems rather hard for him to live without using the substance. The person often suffers such symptoms as withdrawal among other symptoms associated with drug abuse and dependence.






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Amphetamine was used to treat children with
Methylphenidate is currently the most commonly prescribed drug to treat children with attention deficit disorder and is also used to treat narcolepsy. Originally, amphetamine was used to treat children with attention deficit disorder until its addictive potential was recognized. It was estimated in 1992 that 3% of school age children were being treated with Methylphenidate for some extended interval. These numbers have continued to increase. Methylphenidate is not thought to stimulate dopamine synthesis or induce release of dopamine from nerve terminals. The action of Methylphenidate is to block the inward transport of dopamine into the presynaptic terminal, resulting in a prolonged dopamine stimulus.




