Jump to content

Main menu Navigation ●Main page ●Contents ●Current events ●Random article ●About Wikipedia ●Contact us ●Donate Contribute ●Help ●Learn to edit ●Community portal ●Recent changes ●Upload file

Search

●Create account ●Log in ●Create account ● Log in Pages for logged out editors learn more ●Contributions ●Talk

Contents

(Top) 1 See also 2 References

Lerisetron

●فارسی ●Српски / srpski ●Srpskohrvatski / српскохрватски ●Tiếng Việt ●中文 Edit links ●Article ●Talk ●Read ●Edit ●View history Tools Actions ●Read ●Edit ●View history General ●What links here ●Related changes ●Upload file ●Special pages ●Permanent link ●Page information ●Cite this page ●Get shortened URL ●Download QR code ●Wikidata item Print/export ●Download as PDF ●Printable version In other projects ●Wikimedia Commons Appearance From Wikipedia, the free encyclopedia

Lerisetron

Clinical data

Other names

F-0930-RS

None

Identifiers

1-Benzyl-2-piperazin-1-yl-1H-benzimidazole

143257-98-1^N

65997

59389^Y

Q36R82SXRG

ChEMBL56900^Y

CompTox Dashboard (EPA)

DTXSID90162368

Chemical and physical data

C₁₈H₂₀N₄

292.386 g·mol⁻¹

InChI=1S/C18H20N4/c1-2-6-15(7-3-1)14-22-17-9-5-4-8-16(17)20-18(22)21-12-10-19-11-13-21/h1-9,19H,10-14H2^Y

Key:PWWDCRQZITYKDV-UHFFFAOYSA-N^Y

^NY (what is this?) (verify)

Lerisetron (code name F-0930-RS) is a drug which acts as an antagonist at the 5-HT₃ receptor.^[1] It is a potent antiemetic^[2]^[3] and was in clinical trials for the treatment of nausea associated with cancer chemotherapy.^[4]

See also[edit]

5-HT₃ antagonist

References[edit]

^ Orjales A, Mosquera R, Labeaga L, Rodes R (February 1997). "New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation". Journal of Medicinal Chemistry. 40 (4): 586–93. doi:10.1021/jm960442e. PMID 9046349.

^ Gomez-de-Segura IA, Grande AG, De Miguel E (1998). "Antiemetic effects of Lerisetron in radiation-induced emesis in the dog". Acta Oncologica. 37 (7–8): 759–63. doi:10.1080/028418698430160. PMID 10050999.

^ Cooper M, Sologuren A, Valiente R, Smith J (2002). "Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers". Arzneimittel-Forschung. 52 (9): 689–94. doi:10.1055/s-0031-1299952. PMID 12404884. S2CID 24423582.

^ Huckle R (July 2003). "Lerisetron. FAES". Current Opinion in Investigational Drugs. 4 (7): 874–7. PMID 14619411.

Serotonin receptor modulators

Agonists: 8-OH-DPAT

Antidepressants (e.g., etoperidone, hydroxynefazodone, nefazodone, trazodone, triazoledione, vilazodone, vortioxetine)

Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, lurasidone, quetiapine, ziprasidone)

Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone)

Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, lisuride, LSD, methylergometrine (methylergonovine), methysergide, pergolide)

Serotonin (5-HT)

Tryptamines (e.g., 5-CT, 5-MeO-DMT, 5-MT, bufotenin, DMT, indorenate, N-Me-5-HT, psilocin, psilocybin)

Antagonists: Atypical antipsychotics (e.g., iloperidone, risperidone, sertindole)

Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, pindolol, propranolol, tertatolol)

Ergolines (e.g., metergoline)

Metitepine (methiothepin)

MIN-117 (WF-516)

Unknown/unsorted: Acetryptine

Ergolines (e.g., ergometrine (ergonovine))

Agonists: Anpirtoline

Ergolines (e.g., bromocriptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)

Serotonin (5-HT)

Triptans (e.g., avitriptan, donitriptan, eletriptan, sumatriptan, zolmitriptan)

Tryptamines (e.g., 5-BT, 5-CT, 5-MT, DMT)

Antagonists: AR-A000002

Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, tertatolol)

Ergolines (e.g., metergoline)

Metitepine (methiothepin)

Unknown/unsorted: Ergolines (e.g., cabergoline, ergometrine (ergonovine), lisuride)

Agonists: CP-122,288

Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, LSD, methysergide)

Serotonin (5-HT)

Triptans (e.g., almotriptan, avitriptan, donitriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan)

Tryptamines (e.g., 5-BT, 5-CT, 5-Et-DMT, 5-MT, 5-(nonyloxy)tryptamine, DMT)

Antagonists: Alniditan

Ergolines (e.g., metergoline)

Metitepine (methiothepin)

Unknown/unsorted: Acetryptine

Ergolines (e.g., lisuride, lysergol, pergolide)

Agonists: BRL-54443

Ergolines (e.g., methysergide)

Serotonin (5-HT)

Triptans (e.g., eletriptan)

Tryptamines (e.g., tryptamine)

Antagonists: Metitepine (methiothepin)

Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine), lysergol, methylergometrine (methylergonovine)

Agonists: BRL-54443

Ergolines (e.g., bromocriptine, lysergol, methylergometrine (methylergonovine) methysergide)

Serotonin (5-HT)

Triptans (e.g., eletriptan, naratriptan, sumatriptan)

Tryptamines (e.g., 5-MT)

Antagonists: Metitepine (methiothepin)

Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN-NBOH, 2CBFly-NBOMe)

2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)

5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)

α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)

Bromo-DragonFLY

DOx (e.g., DOB, DOC, DOI, DOM)

Ergolines (e.g., 1P-LSD, ALD-52, bromocriptine, cabergoline, ergine (LSA), ergometrine (ergonovine), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, methylergometrine (methylergonovine), pergolide)

MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)

Phenethylamines (e.g., lophophine, mescaline)

Piperazines (e.g., BZP, quipazine, TFMPP)

Serotonin (5-HT)

Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)

Antagonists: 5-I-R91150

Antihistamines (e.g., cyproheptadine, hydroxyzine, ketotifen, perlapine)

Atypical antipsychotics (e.g., amperozide, aripiprazole, asenapine, blonanserin, brexpiprazole, carpipramine, clocapramine, clorotepine, clozapine, fluperlapine, gevotroline, iloperidone, lurasidone, melperone, mosapramine, ocaperidone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, zicronapine, ziprasidone, zotepine)

Chlorprothixene

Ergolines (e.g., amesergide, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)

Metitepine (methiothepin)

MIN-117 (WF-516)

Opiranserin (VVZ-149)

Phenoxybenzamine

Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, triazoledione, trazodone)

Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)

Tricyclic antidepressants (e.g., amitriptyline)

Typical antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, loxapine, perphenazine, pimozide, pipamperone, prochlorperazine, setoperone, spiperone, spiramide, thioridazine, thiothixene, trifluoperazine)

Unknown/unsorted: Ergolines (e.g., dihydroergotamine, nicergoline)

Agonists: 4-Methylaminorex

Amphetamines (e.g., chlorphentermine, cloforex, dexfenfluramine, fenfluramine, levofenfluramine, norfenfluramine)

DOx (e.g., DOB, DOC, DOI, DOM)

Ergolines (e.g., cabergoline, dihydroergocryptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)

MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)

Piperazines (e.g., TFMPP)

Serotonin (5-HT)

Tryptamines (e.g., 5-BT, 5-CT, 5-MT, α-Me-5-HT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)

Antagonists: Agomelatine

Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, N-desalkylquetiapine (norquetiapine), N-desmethylclozapine (norclozapine), olanzapine, pipamperone, quetiapine, risperidone, ziprasidone)

Ergolines (e.g., amesergide, bromocriptine, lisuride, LY-53857, LY-272015, mesulergine)

Metitepine (methiothepin)

Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)

Typical antipsychotics (e.g., chlorpromazine)

Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine))

Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)

5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)

α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)

DOx (e.g., DOB, DOC, DOI, DOM)

Ergolines (e.g., ALD-52, cabergoline, dihydroergotamine, ergine (LSA), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, pergolide)

MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)

Phenethylamines (e.g., lophophine, mescaline)

Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP)

Serotonin (5-HT)

Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)

Antagonists: Adatanserin

Atypical antipsychotics (e.g., asenapine, clorotepine, clozapine, fluperlapine, iloperidone, melperone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, zotepine)

Ergolines (e.g., amesergide, bromocriptine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)

Latrepirdine (dimebolin)

Metitepine (methiothepin)

Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)

Tricyclic antidepressants (e.g., amitriptyline, nortriptyline)

Typical antipsychotics (e.g., chlorpromazine, loxapine, pimozide, pipamperone, thioridazine)

Unknown/unsorted: Efavirenz

Ergolines (e.g., ergometrine (ergonovine), methylergometrine (methylergonovine))

Agonists: Alcohols (e.g., butanol, ethanol (alcohol), trichloroethanol)

Phenylbiguanide

Piperazines (e.g., BZP, mCPP, quipazine)

Serotonin (5-HT)

Tryptamines (e.g., 2-Me-5-HT, 5-CT, bufotenidine (5-HTQ))

Volatiles/gases (e.g., halothane, isoflurane, toluene, trichloroethane)

Antagonists: Alosetron

Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine)

Bemesetron (MDL-72222)

Hydroxybupropion

Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)

Typical antipsychotics (e.g., loxapine)

Volatiles/gases (e.g., nitrous oxide, sevoflurane, xenon)

Unknown/unsorted: LY-53857

Piperazines (e.g., naphthylpiperazine)

Agonists: 5-MT

Serotonin (5-HT)

Antagonists: GR-113808

Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD)

Serotonin (5-HT)

Tryptamines (e.g., 5-CT)

Antagonists: Asenapine

Latrepirdine (dimebolin)

Metitepine (methiothepin)

Unknown/unsorted: Ergolines (e.g., metergoline, methysergide)
Piperazines (e.g., naphthylpiperazine)

Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, methysergide)

Serotonin (5-HT)

Tryptamines (e.g., 2-Me-5-HT, 5-BT, 5-CT, 5-MT, Bufotenin, E-6801, E-6837, EMD-386088, EMDT, LY-586713, N-Me-5-HT, ST-1936, tryptamine)

Antagonists: ABT-354

Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, iloperidone, olanzapine, tiospirone)

Latrepirdine (dimebolin)

Metitepine (methiothepin)

Tetracyclic antidepressants (e.g., amoxapine, mianserin)

Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, nortriptyline)

Typical antipsychotics (e.g., chlorpromazine, loxapine)

Unknown/unsorted: Ergolines (e.g., 2-Br-LSD (BOL-148), bromocriptine, lergotrile, pergolide)

Piperazines (e.g., naphthylpiperazine)

Agonists: 8-OH-DPAT

Ergolines (e.g., LSD)

Serotonin (5-HT)

Triptans (e.g., frovatriptan)

Tryptamines (e.g., 5-CT, 5-MT, bufotenin, N-Me-5-HT)

Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, fluperlapine, olanzapine, risperidone, sertindole, tiospirone, ziprasidone, zotepine)

Ergolines (e.g., 2-Br-LSD (BOL-148), amesergide, bromocriptine, cabergoline, dihydroergotamine, ergotamine, LY-53857, LY-215,840, mesulergine, metergoline, methysergide, sergolexole)

Metitepine (methiothepin)

Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)

Tricyclic antidepressants (e.g., amitriptyline, clomipramine, imipramine)

Typical antipsychotics (e.g., acetophenazine, chlorpromazine, chlorprothixene, fluphenazine, loxapine, pimozide)

Unknown/unsorted: Ergolines (e.g., lisuride, pergolide)

Piperazines (e.g., naphthylpiperazine)

See also: Receptor/signaling modulators

Adrenergics

Dopaminergics

Melatonergics

Monoamine reuptake inhibitors and releasing agents

Monoamine metabolism modulators

Monoamine neurotoxins

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.

t

e

Retrieved from "https://en.wikipedia.org/w/index.php?title=Lerisetron&oldid=1191613754" Categories: ●Drugs not assigned an ATC code ●5-HT3 antagonists ●Antiemetics ●Benzimidazoles ●1-Piperazinyl compounds ●Benzyl compounds ●Gastrointestinal system drug stubs Hidden categories: ●Articles with short description ●Short description matches Wikidata ●Articles with changed CASNo identifier ●Chemical pages without DrugBank identifier ●Articles without KEGG source ●Drugs with no legal status ●Drugboxes which contain changes to verified fields ●Drugboxes which contain changes to watched fields ●All stub articles ●This page was last edited on 24 December 2023, at 16:13 (UTC). ●Text is available under the Creative Commons Attribution-ShareAlike License 4.0; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization. ●Privacy policy ●About Wikipedia ●Disclaimers ●Contact Wikipedia ●Code of Conduct ●Developers ●Statistics ●Cookie statement ●Mobile view