| Term |
Definition |
| blood-brain barrier |
The blood-brain barrier is a physical barrier made up of neuroglia and capillary walls which limits the movement of substances in the bloodstream into the brain. The blood-brain barrier appears to exist primarily to protect the brain from the chemical messenger systems flowing around the body. |
| cannabinoid receptors (CB) |
The cannabinoid receptors are a class of receptors under the G-protein coupled receptor superfamily. Cannabinoid receptors work by inhibiting adenylate cyclase and thereby inhibit production of the second messenger molecule cyclic AMP. They are activated by cannabinoids, found naturally inside the body or introduced as a drug (which may be a synthetic compound or a herbal extract). |
| centrally acting opiates |
Centrally acting opiates are agents that bind to opioid receptors found principally in the central nervous system. There are four broad classes of opioids: endogenous opioid peptides, produced in the body; opium alkaloids, such as morphine (the prototypical opioid) and codeine; semi-synthetic opioids such as heroin and oxycodone; and fully synthetic opioids such as pethidine and methadone that have structures unrelated to the opium alkaloids. |
| centrally-acting mu opioid analgesics |
Centrally-acting mu opioid analgesics are any agents that bind to mu opioid receptors found principally in the central nervous system. |
| diabetic neuropathy |
Diabetic neuropathies are neuropathic disorders that are associated with diabetes mellitus. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (vasa nervorum). Diabetes is the leading cause of neuropathy in developed countries, and neuropathy is the most common complication and greatest source of morbidity and mortality in diabetes patients. It is estimated that the prevalence of neuropathy in diabetes patients is approximately 20%. Diabetic neuropathy is implicated in 50-75% of nontraumatic amputations. |
| dimer |
In recent years, studies have demonstrated that GPCRs (G protein-coupled receptors) can form paired protein complexes – dimers - with other GPCRs on the cell surface. Two of the same GPCRs can pair up to form a homodimer , or two different GPCRs can pair up to form a heterodimer. Compared to the GPCR monomers (single receptors), some of these receptor dimers display new, unexpected drug recognition and response properties, which means that there exists a broad, new array of unexplored drug targets within the GPCR superfamily. |
| G protein-coupled receptor superfamily |
The GPCR superfamily is the largest family of membrane proteins, members of which are involved in all types of stimulus-response pathways, from intercellular communication to physiological senses and consequently, pathological functions. GPCRs are the targets of 40 to 50% of modern medicinal drugs. |
| G protein-coupled receptors (GPCRs) |
G-protein-coupled receptors are transmembrane receptors that transduce an extracellular signal (ligand binding) into an intracellular signal (via G protein activation). GPCRs represent the most successful and therapeutically useful drug targets in modern medicine. |
| heterodimer |
A heterodimer represents two different GPCRs that pair up to form a receptor dimer. Compared to the GPCR monomers (single receptor), some of these receptor dimers display new, unexpected drug recognition and response properties, which means that there exists a broad, new array of unexplored drug targets within the GPCR superfamily. |
| homodimer |
A homodimer represent two identical GPCRs that pair up to form a receptor dimer. |
| kappa agonists |
A kappa agonist (or kappa opioid agonist) is a substance that binds to a kappa opioid receptor and triggers a response in the cell. The receptors of the human body work by being stimulated or inhibited by natural (such as hormones and neurotransmitters) or synthetic (such as drugs) agonists and antagonists. |
| kappa opioid agonist |
A kappa opioid agonist (or kappa agonist) is a substance that binds to a kappa opioid receptor and triggers a response in a cell. The receptors of the human body work by being stimulated or inhibited by natural (such as hormones and neurotransmitters) or synthetic (such as drugs) agonists and antagonists, respectively. |
| kappa opioid receptors |
A kappa opioid receptor is one of the three receptor subtypes ( mu, delta and kappa) that belongs to the family of opioid receptors. |
| ligands |
a ligand is a small molecule that binds to a larger macromolecule. |
| monomer |
Monomer represents a single receptor. |
| non-steroidal anti-inflammatory drugs (NSAIDs) |
NSAIDS are drugs with analgesic, antipyretic and anti-inflammatory effects - they reduce pain, fever and inflammation. The term "non-steroidal" is used to distinguish these drugs from steroids, which (amongst a broad range of other effects) have a similar range of action. The most prominent members of this group of drugs are aspirin and ibuprofen. |
| opioid analgesics |
An opioid is any agent that binds to opioid receptors. |
| peripheral kappa opioid receptor agonists |
Opiate analgesics can act through three different types of opioid receptors, called mu, delta, and kappa. Morphine, the most widely used opiate analgesic, acts primarily via activation of the mu opioid receptor located in the central nervous system (CNS). This CNS action induces pain relief but is also associated with a wide array of CNS-mediated side effects including sedation, respiratory depression, and abuse liability. As a way to avoid these undesirable CNS effects, there has been an effort to develop opioids which selectively activate (agonist) peripheral opioid receptors such as kappa receptors, present on sensory nerves, outside the central nervous system. |
| peripheral kappa receptors |
Peripheral kappa receptors represent kappa opioid receptors localized on sensory nerves, outside of the central nervous system. |
| peripherally acting kappa opioid agonist |
Opiate analgesics can act through three different types of opioid receptors, called mu, delta, and kappa. Morphine, the most widely used opiate analgesic, acts primarily via activation of the mu opioid receptor located in the central nervous system (CNS). This CNS action induces pain relief but is also associated with a wide array of CNS-mediated side effects including sedation, respiratory depression, and abuse liability. As a way to avoid these undesirable CNS effects, there has been an effort to develop peripherally acting opioids which selectively activate peripheral opioid receptors such as kappa receptors, present on sensory nerves, outside the central nervous system. |
| post-herpetic neuralgia |
Post-herpetic neuralgia is a painful, often excruciating condition caused by the damage that the varicella zoster virus causes to the affected nerves during and after an attack of herpes zoster (shingles). It usually manifests itself after the pustules have started to die down. The pain is not controlled by traditional painkillers such as opiates and other analgesics as it is a fundamental (neuropathic) nerve pain. |
| selective cyclo-oxygenase inhibitors |
COX-2 selective inhibitor is a form of NSAID that directly targets COX-2, an enzyme responsible for inflammation and pain. This type of medicine is often used to treat arthritis. |
| transmembrane receptors |
Transmembrane receptors are integral membrane proteins , which reside and operate typically within a cell's plasma membrane, but also in the membranes of some subcellular compartments and organelles. For instance, when a ligand binds to one of these transmembrane receptors on one side of a cellular membrane, a cellular response is initiated on the other side. In this way transmembrane receptors such as GPCRs play a unique and important role in cellular communications and signal transduction. |
| trigeminal neuralgia |
Trigeminal neuralgia, or Tic Douloreux, is a neuropathic disorder of the trigeminal nerve that causes episodes of intense pain in the eyes, lips, nose, scalp, forehead, upper jaw, and lower jaw. Trigeminal neuralgia is considered by most physicians to be the most painful condition known to man, and has, in fact, been called the "suicide disease," because this has been the choice of many people who were unable to have their pain controlled with medications or surgery. An estimated one in 25,000 people suffer from Trigeminal Neuralgia, although the number may be significantly higher, as this disease is often misdiagnosed. |
