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Cannabinoid receptor antagonist

Index Cannabinoid receptor antagonist

A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of cannabinoidergic drug that binds to cannabinoid receptors (CBR) and prevents their activation by endocannabinoids. [1]

96 relations: Adenylyl cyclase, Agonist, Alcohol, Alkane, Alkyl, AM-251 (drug), Amide, Anandamide, Antibody, Autonomic nervous system, Azetidine, Bioavailability, Bioisostere, Blood–brain barrier, Cannabidiol, Cannabinoid, Cannabinoid receptor, Cannabinoid receptor type 1, Cannabinoid receptor type 2, Cannabis (drug), Cannabis sativa, Carbonyl group, Carboxamide, Cyclic adenosine monophosphate, Drug, Eicosanoid, Endocannabinoid enhancer, Endocannabinoid reuptake inhibitor, Endocannabinoid system, Ether, European Medicines Agency, European Union, Fatty acid, G protein–coupled receptor, Haematopoiesis, Halogen, Hashish, Heterocyclic compound, Hydantoin, Hydrazide, Hydrogen bond, Hypothalamus, Ibipinabant, Imidazole, Indazole, Insulin, Inverse agonist, Isostere, Ketone, Merck & Co., ..., Mesolimbic pathway, Mitogen-activated protein kinase, N-Arachidonoyl dopamine, NESS-0327, Neuroendocrine cell, Nicotine withdrawal, Nonsteroidal anti-inflammatory drug, Obesity, Otenabant, Over-the-counter drug, Partial agonist, Pentyl group, Peripheral nervous system, Peristalsis, Pfizer, Pharmacophore, Piperidine, Potassium channel, Pravadoline, Public health, Purine, Pyrazine, Pyrazole, Pyrimidine, Raphael Mechoulam, Receptor antagonist, Rimonabant, Russia, Salt bridge (protein and supramolecular), Sanofi, Sensory nervous system, Smoking cessation, Structure–activity relationship, Sulfonyl, Surinabant, Taranabant, Tetrahydrocannabinol, Tetrahydrocannabivarin, TM-38837, Transmembrane protein, Virodhamine, Vomiting, Weight loss, 1,3-Benzodioxole, 2-Arachidonoylglycerol, 2-Arachidonyl glyceryl ether. Expand index (46 more) »

Adenylyl cyclase

Adenylyl cyclase (also commonly known as adenyl cyclase and adenylate cyclase, abbreviated AC) is an enzyme with key regulatory roles in essentially all cells.

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Agonist

An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.

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Alcohol

In chemistry, an alcohol is any organic compound in which the hydroxyl functional group (–OH) is bound to a carbon.

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Alkane

In organic chemistry, an alkane, or paraffin (a historical name that also has other meanings), is an acyclic saturated hydrocarbon.

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Alkyl

In organic chemistry, an alkyl substituent is an alkane missing one hydrogen.

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AM-251 (drug)

AM-251 is an inverse agonist at the CB1 cannabinoid receptor.

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Amide

An amide (or or), also known as an acid amide, is a compound with the functional group RnE(O)xNR′2 (R and R′ refer to H or organic groups).

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Anandamide

Anandamide, also known as N-arachidonoylethanolamine or AEA, is a fatty acid neurotransmitter derived from the non-oxidative metabolism of eicosatetraenoic acid (arachidonic acid) an essential ω-6 polyunsaturated fatty acid.

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Antibody

An antibody (Ab), also known as an immunoglobulin (Ig), is a large, Y-shaped protein produced mainly by plasma cells that is used by the immune system to neutralize pathogens such as pathogenic bacteria and viruses.

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Autonomic nervous system

The autonomic nervous system (ANS), formerly the vegetative nervous system, is a division of the peripheral nervous system that supplies smooth muscle and glands, and thus influences the function of internal organs.

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Azetidine

Azetidine is a saturated heterocyclic organic compound containing three carbon atoms and one nitrogen atom.

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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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Bioisostere

In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound.

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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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Cannabidiol

Cannabidiol (CBD) is a naturally occurring cannabinoid constituent of cannabis.

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Cannabinoid

A cannabinoid is one of a class of diverse chemical compounds that acts on cannabinoid receptors in cells that alter neurotransmitter release in the brain.

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Cannabinoid receptor

Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system, which is involved in a variety of physiological processes including appetite, pain-sensation, mood, and memory.

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Cannabinoid receptor type 1

The cannabinoid type 1 receptor, often abbreviated as CB1, is a G protein-coupled cannabinoid receptor located in the central and peripheral nervous system.

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Cannabinoid receptor type 2

The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene.

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Cannabis (drug)

Cannabis, also known as marijuana among other names, is a psychoactive drug from the ''Cannabis'' plant intended for medical or recreational use.

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Cannabis sativa

Cannabis sativa is an annual herbaceous flowering plant indigenous to eastern Asia but now of cosmopolitan distribution due to widespread cultivation.

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Carbonyl group

In organic chemistry, a carbonyl group is a functional group composed of a carbon atom double-bonded to an oxygen atom: C.

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Carboxamide

In organic chemistry carboxamides (or amino carbonyls) are functional groups with the general structure R-CO-NR'R′′ with R, R', and R′′ as organic substituents, or hydrogen.

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Cyclic adenosine monophosphate

Cyclic adenosine monophosphate (cAMP, cyclic AMP, or 3',5'-cyclic adenosine monophosphate) is a second messenger important in many biological processes.

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Drug

A drug is any substance (other than food that provides nutritional support) that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes a temporary physiological (and often psychological) change in the body.

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Eicosanoid

Eicosanoids are signaling molecules made by the enzymatic or non-enzymatic oxidation of arachidonic acid or other polyunsaturated fatty acids (PUFAs) that are, similar to arachidonic acid, 20 carbon units in length.

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Endocannabinoid enhancer

An endocannabinoid enhancer (eCBE) is a type of cannabinoidergic drug that enhances the activity of the endocannabinoid system by increasing extracellular concentrations of endocannabinoids.

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Endocannabinoid reuptake inhibitor

Endocannabinoid reuptake inhibitors (eCBRIs), also called cannabinoid reuptake inhibitors (CBRIs), are drugs which limit the reabsorption of endocannabinoid neurotransmitters by the releasing neuron.

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Endocannabinoid system

The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are endogenous lipid-based retrograde neurotransmitters that bind to cannabinoid receptors, and cannabinoid receptor proteins that are expressed throughout the mammalian central nervous system (including the brain) and peripheral nervous system.

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Ether

Ethers are a class of organic compounds that contain an ether group—an oxygen atom connected to two alkyl or aryl groups.

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European Medicines Agency

The European Medicines Agency (EMA) is a European Union agency for the evaluation of medicinal products.

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European Union

The European Union (EU) is a political and economic union of EUnum member states that are located primarily in Europe.

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Fatty acid

In chemistry, particularly in biochemistry, a fatty acid is a carboxylic acid with a long aliphatic chain, which is either saturated or unsaturated.

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G protein–coupled receptor

G protein–coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses.

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Haematopoiesis

Haematopoiesis (from Greek αἷμα, "blood" and ποιεῖν "to make"; also hematopoiesis in American English; sometimes also haemopoiesis or hemopoiesis) is the formation of blood cellular components.

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Halogen

The halogens are a group in the periodic table consisting of five chemically related elements: fluorine (F), chlorine (Cl), bromine (Br), iodine (I), and astatine (At).

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Hashish

Hashish, or hash, is a drug made from cannabis.

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Heterocyclic compound

A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s).

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Hydantoin

Hydantoin, or glycolylurea, is a heterocyclic organic compound with the formula CH2C(O)NHC(O)NH.

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Hydrazide

Hydrazides in organic chemistry are a class of organic compounds sharing a common functional group characterized by a nitrogen to nitrogen covalent bond with 4 substituents with at least one of them being an acyl group.

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Hydrogen bond

A hydrogen bond is a partially electrostatic attraction between a hydrogen (H) which is bound to a more electronegative atom such as nitrogen (N), oxygen (O), or fluorine (F), and another adjacent atom bearing a lone pair of electrons.

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Hypothalamus

The hypothalamus(from Greek ὑπό, "under" and θάλαμος, thalamus) is a portion of the brain that contains a number of small nuclei with a variety of functions.

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Ibipinabant

Ibipinabant (SLV319, BMS-646,256) is a drug used in scientific research which acts as a potent and highly selective CB1 antagonist.

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Imidazole

Imidazole is an organic compound with the formula C3N2H4.

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Indazole

Indazole, also called isoindazole, is a heterocyclic aromatic organic compound.

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Insulin

Insulin (from Latin insula, island) is a peptide hormone produced by beta cells of the pancreatic islets; it is considered to be the main anabolic hormone of the body.

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Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.

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Isostere

Classical Isosteres are molecules or ions with the similar shape and often electronic properties.

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Ketone

In chemistry, a ketone (alkanone) is an organic compound with the structure RC(.

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Merck & Co.

Merck & Company, Inc., d.b.a. Merck Sharp & Dohme (MSD) outside the United States and Canada, is an American pharmaceutical company and one of the largest pharmaceutical companies in the world.

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Mesolimbic pathway

The mesolimbic pathway, sometimes referred to as the reward pathway, is a dopaminergic pathway in the brain.

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Mitogen-activated protein kinase

A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of protein kinase that is specific to the amino acids serine and threonine (i.e., a serine/threonine-specific protein kinase).

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N-Arachidonoyl dopamine

N-Arachidonoyl dopamine (NADA) is an endocannabinoid that acts as an agonist of the CB1 receptor and the transient receptor potential V1 (TRPV1) ion channel.

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NESS-0327

NESS-0327 is a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptor CB1.

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Neuroendocrine cell

Neuroendocrine cells are cells that receive neuronal input (neurotransmitters released by nerve cells or neurosecretory cells) and, as a consequence of this input, release message molecules (hormones) to the blood.

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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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Nonsteroidal anti-inflammatory drug

Nonsteroidal anti-inflammatory drugs (NSAIDs) are a drug class that reduce pain, decrease fever, prevent blood clots and, in higher doses, decrease inflammation.

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Obesity

Obesity is a medical condition in which excess body fat has accumulated to the extent that it may have a negative effect on health.

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Otenabant

Otenabant (CP-945,598) is a drug which acts as a potent and highly selective CB1 antagonist.

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Over-the-counter drug

Over-the-counter (OTC) drugs are medicines sold directly to a consumer without a prescription from a healthcare professional, as opposed to prescription drugs, which may be sold only to consumers possessing a valid prescription.

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Partial agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.

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Pentyl group

In organic chemistry, pentyl is a five-carbon alkyl functional group (substituent) with chemical formula -C5H11.

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Peripheral nervous system

The peripheral nervous system (PNS) is one of the two components of the nervous system, the other part is the central nervous system (CNS).

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Peristalsis

Peristalsis is a radially symmetrical contraction and relaxation of muscles that propagates in a wave down a tube, in an anterograde direction.

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Pfizer

Pfizer Inc. is an American pharmaceutical conglomerate headquartered in New York City, with its research headquarters in Groton, Connecticut.

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Pharmacophore

An example of a pharmacophore model. A pharmacophore is an abstract description of molecular features that are necessary for molecular recognition of a ligand by a biological macromolecule.

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Piperidine

Piperidine is an organic compound with the molecular formula (CH2)5NH.

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Potassium channel

Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms.

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Pravadoline

Pravadoline (WIN 48,098) is an antiinflammatory and analgesic drug with an IC50 of 4.9 µM and a Ki of 2511 nM at CB1, related in structure to nonsteroidal anti-inflammtory drugs (NSAIDs) such as indometacin.

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Public health

Public health is "the science and art of preventing disease, prolonging life and promoting human health through organized efforts and informed choices of society, organizations, public and private, communities and individuals".

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Purine

A purine is a heterocyclic aromatic organic compound that consists of a pyrimidine ring fused to an imidazole ring.

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Pyrazine

Pyrazine is a heterocyclic aromatic organic compound with the chemical formula C4H4N2.

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Pyrazole

Pyrazole is an organic compound with the formula C3H3N2H.

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Pyrimidine

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine.

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Raphael Mechoulam

Raphael Mechoulam (רפאל משולם) (born 1930) is an Israeli organic chemist and professor of Medicinal Chemistry at the Hebrew University of Jerusalem in Israel.

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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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Rimonabant

Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States.

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Russia

Russia (rɐˈsʲijə), officially the Russian Federation (p), is a country in Eurasia. At, Russia is the largest country in the world by area, covering more than one-eighth of the Earth's inhabited land area, and the ninth most populous, with over 144 million people as of December 2017, excluding Crimea. About 77% of the population live in the western, European part of the country. Russia's capital Moscow is one of the largest cities in the world; other major cities include Saint Petersburg, Novosibirsk, Yekaterinburg and Nizhny Novgorod. Extending across the entirety of Northern Asia and much of Eastern Europe, Russia spans eleven time zones and incorporates a wide range of environments and landforms. From northwest to southeast, Russia shares land borders with Norway, Finland, Estonia, Latvia, Lithuania and Poland (both with Kaliningrad Oblast), Belarus, Ukraine, Georgia, Azerbaijan, Kazakhstan, China, Mongolia and North Korea. It shares maritime borders with Japan by the Sea of Okhotsk and the U.S. state of Alaska across the Bering Strait. The East Slavs emerged as a recognizable group in Europe between the 3rd and 8th centuries AD. Founded and ruled by a Varangian warrior elite and their descendants, the medieval state of Rus arose in the 9th century. In 988 it adopted Orthodox Christianity from the Byzantine Empire, beginning the synthesis of Byzantine and Slavic cultures that defined Russian culture for the next millennium. Rus' ultimately disintegrated into a number of smaller states; most of the Rus' lands were overrun by the Mongol invasion and became tributaries of the nomadic Golden Horde in the 13th century. The Grand Duchy of Moscow gradually reunified the surrounding Russian principalities, achieved independence from the Golden Horde. By the 18th century, the nation had greatly expanded through conquest, annexation, and exploration to become the Russian Empire, which was the third largest empire in history, stretching from Poland on the west to Alaska on the east. Following the Russian Revolution, the Russian Soviet Federative Socialist Republic became the largest and leading constituent of the Union of Soviet Socialist Republics, the world's first constitutionally socialist state. The Soviet Union played a decisive role in the Allied victory in World War II, and emerged as a recognized superpower and rival to the United States during the Cold War. The Soviet era saw some of the most significant technological achievements of the 20th century, including the world's first human-made satellite and the launching of the first humans in space. By the end of 1990, the Soviet Union had the world's second largest economy, largest standing military in the world and the largest stockpile of weapons of mass destruction. Following the dissolution of the Soviet Union in 1991, twelve independent republics emerged from the USSR: Russia, Ukraine, Belarus, Kazakhstan, Uzbekistan, Armenia, Azerbaijan, Georgia, Kyrgyzstan, Moldova, Tajikistan, Turkmenistan and the Baltic states regained independence: Estonia, Latvia, Lithuania; the Russian SFSR reconstituted itself as the Russian Federation and is recognized as the continuing legal personality and a successor of the Soviet Union. It is governed as a federal semi-presidential republic. The Russian economy ranks as the twelfth largest by nominal GDP and sixth largest by purchasing power parity in 2015. Russia's extensive mineral and energy resources are the largest such reserves in the world, making it one of the leading producers of oil and natural gas globally. The country is one of the five recognized nuclear weapons states and possesses the largest stockpile of weapons of mass destruction. Russia is a great power as well as a regional power and has been characterised as a potential superpower. It is a permanent member of the United Nations Security Council and an active global partner of ASEAN, as well as a member of the G20, the Shanghai Cooperation Organisation (SCO), the Council of Europe, the Asia-Pacific Economic Cooperation (APEC), the Organization for Security and Co-operation in Europe (OSCE), and the World Trade Organization (WTO), as well as being the leading member of the Commonwealth of Independent States (CIS), the Collective Security Treaty Organization (CSTO) and one of the five members of the Eurasian Economic Union (EEU), along with Armenia, Belarus, Kazakhstan and Kyrgyzstan.

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Salt bridge (protein and supramolecular)

In chemistry, a salt bridge is a combination of two non-covalent interactions: hydrogen bonding and ionic bonding (Figure 1).

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Sanofi

Sanofi S.A. is a French multinational pharmaceutical company headquartered in Gentilly, France, as of 2013 the world's fifth-largest by prescription sales.

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Sensory nervous system

The sensory nervous system is a part of the nervous system responsible for processing sensory information.

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Smoking cessation

Smoking cessation (also known as quitting smoking or simply quitting) is the process of discontinuing tobacco smoking.

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Structure–activity relationship

commented out as it doesn't appear to be immediately relevant & it is in the wrong place if it is relevant-->The structure–activity relationship (SAR) is the relationship between the chemical or 3D structure of a molecule and its biological activity.

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Sulfonyl

A sulfonyl group can refer either to a functional group found primarily in sulfones or to a substituent obtained from a sulfonic acid by the removal of the hydroxyl group similarly to acyl groups.

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Surinabant

Surinabant (SR147778) is a cannabinoid receptor type 1 antagonist developed by Sanofi-Aventis.

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Taranabant

Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 inverse agonist that was investigated as a potential treatment for obesity due to its anorectic effects.

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Tetrahydrocannabinol

Tetrahydrocannabinol (THC) is one of at least 113 cannabinoids identified in cannabis.

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Tetrahydrocannabivarin

Tetrahydrocannabivarin (THCV, THV) is a homologue of tetrahydrocannabinol (THC) having a propyl (3-carbon) side chain instead of a pentyl (5-carbon) group on the molecule, which makes it produce very different effects from THC.

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TM-38837

TM-38837 is a small molecule inverse agonist/antagonist of the CB1 cannabinoid receptor, with peripheral selectivity.

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Transmembrane protein

A transmembrane protein (TP) is a type of integral membrane protein that spans the entirety of the biological membrane to which it is permanently attached.

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Virodhamine

Virodhamine (O-arachidonoyl ethanolamine; O-AEA) is an endocannabinoid and a nonclassic eicosanoid, derived from arachidonic acid.

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Vomiting

Vomiting, also known as emesis, puking, barfing, throwing up, among other terms, is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose.

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Weight loss

Weight loss, in the context of medicine, health, or physical fitness, refers to a reduction of the total body mass, due to a mean loss of fluid, body fat or adipose tissue or lean mass, namely bone mineral deposits, muscle, tendon, and other connective tissue.

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1,3-Benzodioxole

1,3-Benzodioxole (1,2-methylenedioxybenzene) is an organic compound with the formula C6H4O2CH2.

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2-Arachidonoylglycerol

2-Arachidonoylglycerol (2-AG) is an endocannabinoid, an endogenous agonist of the CB1 receptor and the primary endogenous ligand for the CB2 receptor.

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2-Arachidonyl glyceryl ether

2-Arachidonyl glyceryl ether (2-AGE, Noladin ether) is a putative endocannabinoid discovered by Lumír Hanuš and colleagues at the Hebrew University of Jerusalem, Israel.

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Redirects here:

Anti-cannabinoid, Anti-cannabinoids, Anticannabinoid, Anticannabinoids, Cannabinoid Receptor 1 Antagonists: Drug Discovery and Development, Cannabinoid antagonist, Discovery and development of Cannabinoid Receptor 1 Antagonists, Discovery and development of Cannaboid Receptor 1 Antagonists, Endocannabinoid antagonist.

References

[1] https://en.wikipedia.org/wiki/Cannabinoid_receptor_antagonist

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