5-Hydroxytryptamine receptor 2B (5-HT_2B) also known as serotonin receptor 2B is a

protein Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...

that in humans is encoded by the ''HTR2B''

gene In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...

. 5-HT_2B is a member of the 5-HT₂ receptor family that binds the

neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotra ...

serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

(5-hydroxytryptamine, 5-HT). Like all 5-HT₂ receptors, the 5-HT_2B receptor is G_q/G₁₁-protein coupled, leading to downstream activation of

phospholipase C Phospholipase C (PLC) is a class of membrane-associated enzymes that cleave phospholipids just before the phosphate group (see figure). It is most commonly taken to be synonymous with the human forms of this enzyme, which play an important role i ...

Tissue distribution and function

First discovered in the stomach of rats, 5-HT_2B was challenging to characterize initially because of its structural similarity to the other 5-HT₂ receptors, particularly 5-HT_2C. The 5-HT₂ receptors (of which the 5-HT_2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of

. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of

hallucinogen Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mo ...

ic substituted amphetamines. The 5-HT_2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medial amygdala, and meninges. However, its most important role is in the peripheral nervous system (PNS) where it maintains the viability and efficiency of the cardiac valve leaflets. The 5-HT_2B receptor subtype is involved in: * CNS: inhibition of serotonin and dopamine uptake, behavioral effects * Vascular: pulmonary

vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vesse ...

* Cardiac: The 5-HT_2B receptor regulates cardiac structure and functions, as demonstrated by the abnormal cardiac development observed in 5-HT_2B receptor null mice. Excessive stimulation of this receptor causes pathological proliferation of cardiac valve fibroblasts, with chronic overstimulation leading to valvulopathy. These receptors are also overexpressed in human failing heart and antagonists of 5-HT_2B receptors were discovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse. *

Serotonin transporter The serotonin transporter (SERT or 5-HTT) also known as the sodium-dependent serotonin transporter and solute carrier family 6 member 4 is a protein that in humans is encoded by the SLC6A4 gene. SERT is a type of monoamine transporter protein t ...

: 5-HT_2B receptors regulate serotonin release via the serotonin transporter, and are important both to normal physiological regulation of serotonin levels in blood plasma, and with the abnormal acute serotonin release produced by drugs such as

MDMA 3,4-Methylenedioxymethamphetamine (MDMA), commonly known as ecstasy (tablet form), and molly (crystal form), is an empathogen–entactogenic drug with stimulant and minor Psychedelic drug, psychedelic properties. In studies, it has been used ...

. Surprisingly, however, 5-HT_2B receptor activation appears to be protective against the development of

serotonin syndrome Serotonin syndrome (SS) is a group of symptoms that may occur with the use of certain Serotonin, serotonergic medications or Recreational drug use, drugs. The symptoms can range from mild to severe, and are potentially fatal. Symptoms in mild c ...

following elevated extracellular serotonin levels, despite its role in modulating serotonin release.

Clinical significance

Valvular heart disease

5-HT_2B receptors have been strongly implicated in causing drug-induced

valvular heart disease Valvular heart disease is any cardiovascular disease process involving one or more of the four valves of the heart (the aortic and mitral valves on the left side of heart and the pulmonic and tricuspid valves on the right side of heart). The ...

. The

Fen-Phen The medication, drug combination fenfluramine/phentermine, usually called fen-phen, is an anti-obesity medication that is no longer widely available. It was sold in the early 1990s, and utilized two anorectics. Fenfluramine was marketed by Americ ...

scandal in the 80s and 90s revealed the cardiotoxic effects of 5-HT_2B stimulation. Today, 5-HT_2B agonism is considered a toxicity signal precluding further clinical development of a compound.

Migraines

The non-selective serotonin receptor agonist ''meta''-chlorophenylpiperazine (mCPP) induces migraines and this may be due to serotonin 5-HT_2B receptor agonism. Serotonin 5-HT₂ receptor antagonists used as antimigraine agents, such as methysergide,

cyproheptadine Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine, first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It was patented in 1959 a ...

, and pizotifen, may be producing their antimigraine effects specifically via serotonin 5-HT_2B receptor antagonism.

Ligands

The structure of the 5-HT_2B receptor was resolved in a complex with the valvulopathogenic drug

ergotamine Ergotamine, sold under the brand name Ergomar among others, is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is structurally similar to several neurotransmitter ...

.; As of 2009, few highly selective 5-HT_2B receptor ligands have been discovered, although numerous potent non-selective compounds are known, particularly agents with concomitant 5-HT_2C binding. Research in this area has been limited due to the cardiotoxicity of 5-HT_2B agonists, and the lack of clear therapeutic application for 5-HT_2B antagonists, but there is still a need for selective ligands for scientific research.

Agonists

Endogenous

* 5-Methoxytryptamine (5-MT) – trace amine * DMT – trace amine *

Serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

– neurotransmitter, K_D ≈ 10nM *

Tryptamine Tryptamine is an indolamine metabolite of the essential amino acid tryptophan. The chemical structure is defined by an indole—a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the firs ...

– trace amine

Selective

* 6-APB – ~100-fold selectivity over the 5-HT_2A and 5-HT_2C receptors, ≥32-fold selectivity over monoamine release, ~12-fold selectivity over α_2C-adrenergic receptor * α-Methylserotonin – ~10-fold selectivity over 5-HT_2A and 5-HT_2C * BW-723C86 – 100-fold selectivity over 5-HT_2A but only 3- to 10-fold selectivity over 5-HT_2C, fair functional subtype selectivity, almost full agonist, anxiolytic ''in vivo'' * LY-266,097 – biased partial agonist in favor of G_q protein, no β-arrestin2 recruitment * VU6067416 – modest selectivity over 5-HT_2A and 5-HT_2C

Non-selective

* 25C-NBOMe *

25I-NBOMe 25I-NBOMe, also known as 2C-I-NBOMe, Cimbi-5, and shortened to "25I", is a psychedelic drug of the phenethylamine, 2C, and NBOMe (25-NB) families. Since 2010, it has circulated in the recreational drug scene, often misrepresented as LSD. It is ...

* 2C-B * 2C-B-FLY *

2C-C 2C-C is a psychedelic drug of the 2C family. It was first synthesized by Alexander Shulgin, sometimes used as an entheogen. In his book '' PiHKAL (Phenethylamines i Have Known And Loved)'', Shulgin lists the dosage range as 20–40 mg. 2C- ...

2C-D 2C-D, also known as 2C-M or as 2,5-dimethoxy-4-methylphenethylamine, is a psychedelic drug of the 2C family that is sometimes used as an entheogen. It was first synthesized in 1970 by a team from the Texas Research Institute of Mental Sciences, a ...

2C-E 2C-E is a Psychedelic drug, psychedelic phenethylamines, phenethylamine of the 2C (psychedelics), 2C family. It was first synthesized by Alexander Shulgin and documented in his book ''PiHKAL''. Like the other substances in its family, it produces ...

2C-I 2C-I, also known as 2,5-dimethoxy-4-iodophenethylamine, is a phenethylamine of the 2C family with psychedelic effects. It was first synthesized by Alexander Shulgin, and is described in Shulgin's book ''PiHKAL'' (1991). The substance is con ...

* 4-Methylamphetamine * 5-APB * 5-APDB * 5-Carboxamidotryptamine * 5-MAPB * 6-APB * 6-APDB * 6-MAPB * 5-MeO-αMT *

5-MeO-DiPT 5-MeO-DiPT, also known as 5-methoxy-''N'',''N''-diisopropyltryptamine and sometimes as foxy methoxy or simply foxy, is a psychedelic drug of the tryptamine and 5-methoxytryptamine families. It is the 5-methoxy derivative of diisopropyltryptami ...

5-MeO-DMT 5-MeO-DMT (5-methoxy-''N'',''N''-dimethyltryptamine), also known as ''O''-methylbufotenin or mebufotenin (), is a naturally occurring psychedelic of the tryptamine family. It is found in a wide variety of plant species, and is also secreted by ...

* 5-MeO-MiPT * AL-38022A * Aminorex (weakly) *

Ariadne In Greek mythology, Ariadne (; ; ) was a Cretan princess, the daughter of King Minos of Crete. There are variations of Ariadne's myth, but she is known for helping Theseus escape from the Minotaur and being abandoned by him on the island of N ...

Benfluorex Benfluorex, sold under the brand name Mediator, is an anorectic and hypolipidemic agent that is structurally related to fenfluramine (a substituted amphetamine). It may improve glycemic control and decrease insulin resistance in people with ...

* Bromo-dragonfly * Bromocriptine * Cabergoline * Chlorphentermine (very weakly) * CYB210010 (2C-T-TFM) *

Dexfenfluramine Dexfenfluramine, formerly sold under the brand name Redux, is a Serotonin, serotonergic drug that was used as an appetite suppressant to promote weight loss. It is the d-enantiomer of fenfluramine and is structurally similar to amphetamine, but ...

* Dexnorfenfluramine * Dihydroergocryptine * Dihydroergotamine * DiPT *

DOB DOB or Dob often refers to date of birth. DOB or Dob may also refer to: Biochemistry * 2,5-dimethoxy-4-bromoamphetamine, Bromo-DMA, a psychedelic drug ** Meta-DOB, related substance ** Methyl-DOB, related substance * HLA-DOB, human gene Organiz ...

* DOC * DOET * DOI * DOM * Ergometrine (ergonovine) *

Ergotamine Ergotamine, sold under the brand name Ergomar among others, is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is structurally similar to several neurotransmitter ...

Fenfluramine Fenfluramine, sold under the brand name Fintepla, is a serotonergic medication used for the treatment of seizures associated with Dravet syndrome and Lennox–Gastaut syndrome. It was formerly used as an appetite suppressant in the treat ...

* Fenoldopam *

Guanfacine Guanfacine, sold under the brand name Tenex ( immediate-release) and Intuniv ( extended-release) among others, is an oral alpha-2a agonist medication used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure. Co ...

– an α_2A-adrenergic agonist, but has 5-HT_2B agonistic activity at therapeutic concentrations *

Levofenfluramine Levofenfluramine ( INN), or (−)-3-trifluoromethyl-''N''-ethylamphetamine, also known as (−)-fenfluramine or (''R'')-fenfluramine, is a drug of the amphetamine family that, itself (i.e., in enantiopure form), was never marketed alone. It is ...

* Levonorfenfluramine * Lorcaserin *

LSD Lysergic acid diethylamide, commonly known as LSD (from German ; often referred to as acid or lucy), is a semisynthetic, hallucinogenic compound derived from ergot, known for its powerful psychological effects and serotonergic activity. I ...

– about equal affinity for human cloned 5-HT_2B and 5-HT_2A receptors *

LSM-775 LSM-775, also known as ''N''-morpholinyllysergamide or as lysergic acid morpholide, is a chemical derivative, derivative of ergine (lysergamide). It is less potent than lysergic acid diethylamide (LSD) but is reported to have some LSD-like effec ...

* mCPP (in humans; weak partial agonist) * MDA *

* MEM *

Mescaline Mescaline, also known as mescalin or mezcalin, and in chemical terms 3,4,5-trimethoxyphenethylamine, is a natural product, naturally occurring psychedelic drug, psychedelic alkaloid, protoalkaloid of the substituted phenethylamine class, found ...

Methylergometrine Methylergometrine, also known as methylergonovine and sold under the brand name Methergine, is a medication of the ergoline and lysergamide groups which is used as an oxytocic in obstetrics and as an antimigraine agent in the treatment of mi ...

(methylergonovine) * Methysergide (antagonist in some studies) * Naphthylaminopropane * Norfenfluramine * ORG-12962 * ORG-37684 * Oxymetazoline * Pergolide *

PNU-22394 PNU-22394 is a drug of the ibogalog group which acts as an agonist at serotonin 5-HT2 Receptor (biochemistry), receptors, with strongest binding affinity for 5-HT2A receptor, 5-HT2A and 5-HT2C receptor, 5-HT2C and slightly weaker at 5-HT2B recept ...

Psilocin Psilocin, also known as 4-hydroxy-''N'',''N''-dimethyltryptamine (4-HO-DMT), is a substituted tryptamine alkaloid and a serotonergic psychedelic. It is present in most psychedelic mushrooms together with its phosphorylated counterpart psilocy ...

Psilocybin Psilocybin, also known as 4-phosphoryloxy-''N'',''N''-dimethyltryptamine (4-PO-DMT), is a natural product, naturally occurring tryptamine alkaloid and Investigational New Drug, investigational drug found in more than List of psilocybin mushroom ...

* Quipazine (weak partial agonist) * Ro60-0175 – functionally selective over 5-HT_2A, potent agonist at both 5-HT_2B/C * Ropinirole *

Quinidine Quinidine is a class I antiarrhythmic agent, class IA antiarrhythmic agent used to treat heart rhythm disturbances. It is a diastereomer of Antimalarial medication, antimalarial agent quinine, originally derived from the bark of the cinchona tre ...

* TFMPP (weak partial agonist) *

VER-3323 VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C serotonin Receptor (biochemistry), receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT ...

– mixed 5-HT_2C and 5-HT_2B agonist with weaker 5-HT_2A affinity * Xylometazoline

Peripherally selective

* AL-34662 – non-selective over 5-HT_2A and 5-HT_2C

Inactive

A number of notable drugs appear to be inactive or very weak as serotonin 5-HT_2B receptor agonists, at least ''

in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in ...

''. These include the

stimulant Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, ...

s and/or

entactogen Entactogens, also known as empathogens or connectogens, are a class of psychoactive drugs that induce the production of experiences of emotional communion, oneness, connectedness, emotional openness—that is, empathy—as particularly observe ...

dextroamphetamine Dextroamphetamine (international nonproprietary name, INN: dexamfetamine) is a potent central nervous system (CNS) stimulant and enantiomer of amphetamine that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and narc ...

, dextromethamphetamine,

4-fluoroamphetamine 4-Fluoroamphetamine (4-FA; 4-FMP; PAL-303; "Flux"), also known as ''para''-fluoroamphetamine (PFA) is a psychoactive drug, psychoactive research chemical of the phenethylamine and substituted amphetamine chemical classes. It produces stimulant a ...

, 4-fluoromethamphetamine,

phentermine Phentermine, sold under the brand name Adipex-P among others, is a medication used together with diet and exercise to treat obesity. It is available by itself or as the combination phentermine/topiramate. Phentermine is taken by mouth. Com ...

methylone Methylone, also known as 3,4-methylenedioxy-''N''-methylcathinone (MDMC), is an entactogen and stimulant drug of the amphetamine, cathinone, and benzodioxole families related to 3,4-methylenedioxymethamphetamine (MDMA; "ecstasy"). It is th ...

, mephedrone, MDAI, and MMAI, among others. Findings are somewhat conflicting for certain psychedelics, such as

psilocin Psilocin, also known as 4-hydroxy-''N'',''N''-dimethyltryptamine (4-HO-DMT), is a substituted tryptamine alkaloid and a serotonergic psychedelic. It is present in most psychedelic mushrooms together with its phosphorylated counterpart psilocy ...

and

, but most studies find that these drugs are indeed potent serotonin 5-HT_2B receptor agonists.

Antagonists

Selective

* 5-HCPC * 5-HPEC (weak) * 5-HPPC * AM1125 * AM1476 * BF-1 – derived from pimethixene * EGIS-7625 – high selectivity over 5-HT_2A * EXT5 – highly selective * EXT9 – somewhat selective * LY-23,728 * LY-266,097 – pK_i = 9.7, 100-fold selectivity over 5-HT_2A and 5-HT_2C * LY-272,015 – fairly selective and highly potent * LY-287,375 * MRS7925 – substantially selective over 5-HT_2A and 5-HT_2C but minimal selectivity over the

adenosine Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. The molecule consists of an adenine attached to a ribose via a β-N9- glycosidic bond. Adenosine is one of the four nucleoside build ...

A₁ receptor * MRS8209 * MW071 (MW01-8-071HAB) – non-MAOI minaprine analogue * MW073 – highly selective, orally bioavailable * PRX-08066 – K_i ≈ 1.7nM, >100-fold selectivity * RQ-00310941 (RQ-941) – K_i = 2.0nM, IC₅₀ = 17nM, >2,000-fold selectivity against >60 targets, under development for medical use * RS-127,445 (MT-500) – K_i = 0.3nM, >1,000-fold selectivity over 5-HT_2A and 5-HT_2C and numerous other targets, selective over at least eight other serotonin receptors, developed for clinical use but discontinued * SB-204,741 – >135-fold selectivity over 5-HT_2C and 5-HT_2A * SB-215,505 – mixed 5-HT_2B and 5-HT_2C antagonist * VU6047534 – weak partial agonist or antagonist, peripherally selective in mice but not humans

Non-selective

* 2-Bromo-LSD (BOL-148; bromolysergide) * (–)-MBP – 5-HT_2A antagonist, 5-HT_2B inverse agonist, and 5-HT_2C agonist * Agomelatine – primarily a

melatonin Melatonin, an indoleamine, is a natural compound produced by various organisms, including bacteria and eukaryotes. Its discovery in 1958 by Aaron B. Lerner and colleagues stemmed from the isolation of a substance from the pineal gland of cow ...

MT₁/MT₂ receptor agonist, with a less potent antagonism of 5-HT_2B and 5-HT_2C * AMAP102 (AMAP-102) – 5-HT_2B and 5-HT_2C antagonist * Amesergide (LY-237733) *

Amisulpride Amisulpride, sold under the brand names Socian and Barhemsys, is a medication used in the treatment of schizophrenia, acute psychotic episodes, depression, and nausea and vomiting. It is specifically used at lower doses intravenously to prev ...

Amitriptyline Amitriptyline, sold under the brand name Elavil among others, is a tricyclic antidepressant primarily used to treat major depressive disorder, and a variety of pain syndromes such as neuropathic pain, fibromyalgia, migraine and tension headac ...

* Apomorphine *

Aripiprazole Aripiprazole, sold under the brand name Abilify, among others, is an atypical antipsychotic primarily used in the treatment of schizophrenia, bipolar disorder, and irritability associated with autism spectrum disorder; other uses include as ...

Asenapine Asenapine, sold under the brand name Saphris among others, is an atypical antipsychotic medication used to treat schizophrenia and acute mania associated with bipolar disorder as well as the medium to long-term management of bipolar disorder. I ...

* BMB-201 – and active form BMB-39a * Brexpiprazole * Brilaroxazine * C-122 *

Cariprazine Cariprazine, sold under the brand name Vraylar among others, is an atypical antipsychotic developed by Gedeon Richter, which is used in the treatment of schizophrenia and bipolar disorder. It is also prescribed as an add-on treatment for bip ...

Chlorpromazine Chlorpromazine (CPZ), marketed under the brand names Thorazine and Largactil among others, is an antipsychotic medication. It is primarily used to treat psychotic disorders such as schizophrenia. Other uses include the treatment of bipolar d ...

Clozapine Clozapine, sold under the brand name Clozaril among others, is a psychiatric medication and was the first atypical antipsychotic to be discovered. It is used primarily to treat people with schizophrenia and schizoaffective disorder who have ...

Cyproheptadine Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine, first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It was patented in 1959 a ...

* Desmethylclozapine (NDMC; norclozapine) * Ibogainalog * ITI-1549 * KB-128 – 5-HT_2A and 5-HT_2B antagonist and 5-HT_2C agonist * Lisuride – a

dopamine agonist A dopamine agonist is a compound that activates dopamine receptors. There are two families of dopamine receptors, D1-like and D2-like. They are all G protein-coupled receptors. D1- and D5-receptors belong to the D1-like family and the D2-like ...

of the ergoline class, that is also a 5-HT_2B antagonist and a dual 5-HT_2A/C agonist * Lurasidone * LY-53857 * Mesulergine * Metadoxine – a 5-HT_2B antagonist and GABA-activity modulator * Metergoline * Metitepine (methiothepin) * Mianserin * Molindone * ''N''-Methylamisulpride * Nantenine * Naphthylpiperazine (1-NP) *

Olanzapine Olanzapine, sold under the brand name Zyprexa among others, is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. It is also sometimes used off-label for treatment of chemotherapy-induced nausea and vomitin ...

* Pimethixene * Pipamperone * Pizotifen (pizotyline) *

Promethazine Promethazine, sold under the brand name Phenergan among others, is a first-generation antihistamine, sedative, and antiemetic used to treat allergies, insomnia, and nausea. It may also help with some symptoms associated with the common cold a ...

* Quetiapine * Rauwolscine *

Risperidone Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder, as well as aggressive and self-injurious behaviors associated with autism spectrum disorder. It is t ...

Ritanserin Ritanserin, also known by its developmental code name R-55667, is a serotonin receptor antagonist, serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was chiefly inve ...

* SB-200,646 – 5-HT_2B/5-HT_2C antagonist, selective over 5-HT_2A * SB-206,553 – mixed 5-HT_2B and 5-HT_2C antagonist and PAM at α₇ nAChR * SB-221,284 – 5-HT_2B/5-HT_2C antagonist * SB-228,357 – 5-HT_2B/5-HT_2C antagonist * SDZ SER-082 – a mixed 5-HT_2B/C antagonist *

Spiperone Spiperone, also known as spiroperidol and sold under the brand name Spiropitan (( JP)) is a typical antipsychotic of the butyrophenone family related to haloperidol. It is approved for clinical use in Japan as a treatment for schizophrenia. Pha ...

* Tabernanthalog (TBG; DLX-007) * Tegaserod – primarily a 5-HT₄ agonist, but also a 5-HT_2B antagonist * Terguride – an oral, potent antagonist of 5-HT_2A and 5-HT_2B receptors *

Trazodone Trazodone is an antidepressant medication used to treat major depressive disorder, anxiety disorders, and insomnia. It is a phenylpiperazine compound of the serotonin antagonist and reuptake inhibitor (SARI) class. The medication is taken or ...

* Vabicaserin * Viloxazine – weak 5-HT_2B antagonist and 5-HT_2C agonist * Xanomeline – similar affinity as for muscarinic acetylcholine receptors *

Yohimbine Yohimbine, also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe'' (yohimbe); also from the bark of the unrelated South American tree '' Aspidosperma quebracho-blanco''. Yohimbine is ...

* Zalsupindole (DLX-001; AAZ-A-154) * Ziprasidone

Unknown or unsorted selectivity

* AM1030 (AM-1030) * TN-002

Peripherally selective

* MRS8209 * Sarpogrelate (MCI-9042, LS-187,118) – non-selective 5-HT₂ antagonist, but ~2 orders of magnitude lower affinity at 5-HT_2B than at 5-HT_2A * VU0530244 – 5-HT_2B-selective * VU0631019 – 5-HT_2B-selective * VU6055320 – 5-HT_2B-selective * Others (e.g., "compound 19c") BW-501C67 and xylamidine are known peripherally selective antagonists of the serotonin 5-HT₂ receptors, including of the serotonin 5-HT_2A and 5-HT_2B receptors, but their serotonin 5-HT_2B receptor interactions do not appear to have been described.

Possible applications

5-HT_2B antagonists have previously been proposed as treatment for

migraine Migraine (, ) is a complex neurological disorder characterized by episodes of moderate-to-severe headache, most often unilateral and generally associated with nausea, and light and sound sensitivity. Other characterizing symptoms may includ ...

headaches, and RS-127,445 was trialled in humans up to Phase I for this indication, but development was not continued. More recent research has focused on possible application of 5-HT_2B antagonists as treatments for chronic

heart disease Cardiovascular disease (CVD) is any disease involving the heart or blood vessels. CVDs constitute a class of diseases that includes: coronary artery diseases (e.g. angina pectoris, angina, myocardial infarction, heart attack), heart failure, ...

. Research claims serotonin 5-HT_2B receptors have effect on liver regeneration. Antagonism of 5-HT_2B may attenuate fibrogenesis and improve liver function in disease models in which fibrosis is pre-established and progressive.

References

External links

* * * {{DEFAULTSORT:5-Ht2b Receptor Serotonin receptors

Tissue distribution and function

Clinical significance

Valvular heart disease

Migraines

Ligands

Agonists

Endogenous

Selective

Non-selective

Peripherally selective

Inactive

Antagonists

Selective

Non-selective

Unknown or unsorted selectivity

Peripherally selective

Possible applications

See also

References

Further reading

External links