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CERC-501

Index CERC-501

CERC-501 (originally known as LY-2456302) is a selective antagonist of the κ-opioid receptor (KOR) which was originally developed by Eli Lilly and is now under development by Janssen Pharmaceuticals for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence. [1]

38 relations: Absorption (pharmacology), Adjuvant therapy, Alcoholism, Antidepressant, Binding selectivity, Bioavailability, Biological half-life, Blood–brain barrier, Chain smoking, Citalopram, Clinical trial, Cmax (pharmacology), Depression (mood), Eli Lilly, Esketamine, Fentanyl, Illegal drug trade, Imipramine, Δ-opioid receptor, Κ-opioid receptor, Μ-opioid receptor, Janssen Pharmaceutica, List of investigational antidepressants, Major depressive disorder, Miosis, Model organism, Nicotine, Nicotine withdrawal, Oral administration, Pharmacokinetics, Phases of clinical research, Positron emission tomography, Potency (pharmacology), Receptor antagonist, Side effect, Substance dependence, Substance use disorder, Treatment-resistant depression.

Absorption (pharmacology)

In pharmacology (and more specifically pharmacokinetics), absorption is the movement of a drug from the site of administration to bloodstream.

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Adjuvant therapy

Adjuvant therapy, also known as adjunct therapy, add-on therapy, and adjuvant care, is therapy that is given in addition to the primary or initial therapy to maximize its effectiveness.

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Alcoholism

Alcoholism, also known as alcohol use disorder (AUD), is a broad term for any drinking of alcohol that results in mental or physical health problems.

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Antidepressant

Antidepressants are drugs used for the treatment of major depressive disorder and other conditions, including dysthymia, anxiety disorders, obsessive–compulsive disorder, eating disorders, chronic pain, neuropathic pain and, in some cases, dysmenorrhoea, snoring, migraine, attention-deficit hyperactivity disorder (ADHD), addiction, dependence, and sleep disorders.

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Binding selectivity

Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex.

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Bioavailability

In pharmacology, bioavailability (BA or F) is a subcategory of absorption and is the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs.

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Biological half-life

The biological half-life of a biological substance is the time it takes for half to be removed by biological processes when the rate of removal is roughly exponential.

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Blood–brain barrier

The blood–brain barrier (BBB) is a highly selective semipermeable membrane barrier that separates the circulating blood from the brain and extracellular fluid in the central nervous system (CNS).

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Chain smoking

Chain smoking is the practice of smoking several cigarettes in succession, sometimes using the ember of a finished cigarette to light the next.

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Citalopram

Citalopram (brand names: Celexa, Cipramil and others) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class.

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Clinical trial

Clinical trials are experiments or observations done in clinical research.

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Cmax (pharmacology)

Cmax is the maximum (or peak) serum concentration that a drug achieves in a specified compartment or test area of the body after the drug has been administrated and before the administration of a second dose.

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Depression (mood)

Depression is a state of low mood and aversion to activity that can affect a person's thoughts, behavior, tendencies, feelings, and sense of well-being.

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Eli Lilly

Eli Lilly (July 8, 1838 – June 6, 1898) was an American soldier, pharmacist, chemist, and businessman who founded the Eli Lilly and Company pharmaceutical corporation.

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Esketamine

Esketamine, also known as (S)-ketamine or S(+)-ketamine and sold under the brand names Ketanest and Ketanest S among others, is a general anesthetic and a dissociative hallucinogen.

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Fentanyl

Fentanyl, also spelled fentanil, is an opioid which is used as a pain medication and together with other medications for anesthesia. Fentanyl is also made illegally and used as a recreational drug, often mixed with heroin or cocaine. It has a rapid onset and effects generally last less than an hour or two. Medically, fentanyl is used by injection, as a patch on the skin, as a nasal spray, or in the mouth. Common side effects include vomiting, constipation, sedation, confusion, hallucinations, and injuries related to poor coordination. Serious side effects may include decreased breathing (respiratory depression), serotonin syndrome, low blood pressure, addiction, or coma. In 2016, more than 20,000 deaths occurred in the United States due to overdoses of fentanyl and fentanyl analogues, half of all reported opioid related deaths. Fentanyl works primarily by activating μ-opioid receptors. It is around 100 times stronger than morphine, and some analogues such as carfentanil are around 10,000 times stronger. Fentanyl was first made by Paul Janssen in 1960 and approved for medical use in the United States in 1968.In 2015, were used in healthcare globally., fentanyl was the most widely used synthetic opioid in medicine. Fentanyl patches are on the WHO List of Essential Medicines, the most effective and safe medicines needed in a health system. For a 100 microgram vial, the average wholesale cost in the developing world is 0.66 (2015). and in the USA it costs 0.49 (2017).

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Illegal drug trade

The illegal drug trade or drug trafficking is a global black market dedicated to the cultivation, manufacture, distribution and sale of drugs that are subject to drug prohibition laws.

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Imipramine

Imipramine, sold under the brand name Tofranil among others, is a tricyclic antidepressant (TCA) which is used mainly in the treatment of depression.

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Δ-opioid receptor

The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands.

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Κ-opioid receptor

The κ-opioid receptor (KOR) is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene.

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Μ-opioid receptor

The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins.

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Janssen Pharmaceutica

Janssen Pharmaceutica is a pharmaceutical company headquartered in Beerse, Belgium.

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List of investigational antidepressants

This is a list of investigational antidepressants, or antidepressants that are currently under development for clinical use in the treatment of mood disorders but are not yet approved.

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Major depressive disorder

Major depressive disorder (MDD), also known simply as depression, is a mental disorder characterized by at least two weeks of low mood that is present across most situations.

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Miosis

Miosis is excessive constriction of the pupil.

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Model organism

A model organism is a non-human species that is extensively studied to understand particular biological phenomena, with the expectation that discoveries made in the organism model will provide insight into the workings of other organisms.

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Nicotine

Nicotine is a potent parasympathomimetic stimulant and an alkaloid found in the nightshade family of plants.

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Nicotine withdrawal

Nicotine withdrawal is a group of symptoms that occur in the first few weeks upon the abrupt discontinuation or decrease in intake of nicotine.

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Oral administration

| name.

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Pharmacokinetics

Pharmacokinetics (from Ancient Greek pharmakon "drug" and kinetikos "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered to a living organism.

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Phases of clinical research

The phases of clinical research are the steps in which scientists do experiments with a health intervention in an attempt to find enough evidence for a process which would be useful as a medical treatment.

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Positron emission tomography

Positron-emission tomography (PET) is a nuclear medicine functional imaging technique that is used to observe metabolic processes in the body as an aid to the diagnosis of disease.

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Potency (pharmacology)

In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Side effect

In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug.

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Substance dependence

Substance dependence also known as drug dependence is an adaptive state that develops from repeated drug administration, and which results in withdrawal upon cessation of drug use.

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Substance use disorder

A substance use disorder (SUD), also known as a drug use disorder, is a condition in which the use of one or more substances leads to a clinically significant impairment or distress.

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Treatment-resistant depression

Treatment-resistant depression (TRD) or treatment-refractory depression is a term used in clinical psychiatry to describe cases of major depressive disorder (MDD) that do not respond adequately to appropriate courses of at least two antidepressants.

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Redirects here:

C26H27FN2O2, LY 2456302, LY-2456302, LY2456302.

References

[1] https://en.wikipedia.org/wiki/CERC-501

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