Serotonin 5-HT2 Receptor Agonists

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.
DrugDrug NameDrug Indication
DB00574FenfluramineFor the management of exogenous obesity as a short-term (a few weeks) adjunct in a regimen of weight reduction based on caloric restriction.
DB01186PergolideIndicated as adjunctive treatment to levodopa/carbidopa in the management of the signs and symptoms of Parkinson's disease. It was withdrawn from the US and Canadian markets in 2007 due to an increased risk of cardiac valvulopathy.
DB01200BromocriptineFor the treatment of galactorrhea due to hyperprolactinemia, prolactin-dependent menstrual disorders and infertility, prolactin-secreting adenomas, prolactin-dependent male hypogonadism, as adjunct therapy to surgery or radiotherapy for acromegaly or as monotherapy is special cases, as monotherapy in early Parksinsonian Syndrome or as an adjunct with levodopa in advanced cases with motor complications. Bromocriptine has also been used off-label to treat restless legs syndrome and neuroleptic malignant syndrome.
DB00248CabergolineFor the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.
DB00320DihydroergotamineFor the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes.
DB01454MidomafetamineClinical trials are now testing the therapeutic potential of MDMA for post-traumatic stress disorder (PTSD) and anxiety associated with terminal cancer. MDMA is one of the four most widely used illicit drugs in the U.S.
DB04829Lysergic acid diethylamideNot Available
DB00696ErgotamineFor use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".
DB01442MMDAMMDA is a recreational drug. It has no current medical uses and is a Schedule I controlled substance in the USA at present.
DB139402,5-Dimethoxy-4-ethylthioamphetamineNot Available
DB13948N-(2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamineNot Available
DB140105-methoxy-N,N-dimethyltryptamineNot Available
DB12110m-ChlorophenylpiperazineNot Available
DB04948LofexidineLofexidine is indicated for mitigation of symptoms associated with acute withdrawal from opioids and for facilitation of the completion of opioid discontinuation treatment. It is the first non-opioid medication for the symptomatic management of opioid discontinuation.[L2801] Opioid withdrawal syndrome is a debilitating manifestation of opioid dependence.[A33085] This condition is extremely unpleasant lasting several days with some of the main features being abdominal pain, nausea, diarrhea, mydriasis, lacrimation, and piloerection. These symptoms are often observed after abrupt reductions in the opioid dose and can be resolved by re-administration of the opioid.[A33088]
DB09061CannabidiolWhen used in combination with delta-9-tetrahydrocannabinol as the product Sativex, cannabidiol was given a standard marketing authorization (ie. a Notice of Compliance (NOC)) by Health Canada for the following indications: 1) as adjunctive treatment for symptomatic relief of spasticity in adult patients with multiple sclerosis (MS) who have not responded adequately to other therapy and who demonstrate meaningful improvement during an initial trial of therapy [L886]; Due to the need for confirmatory studies to verify the clinical benefit coupled with the promising nature of the clinical evidence, Sativex was also given a Notice of Compliance with Conditions (NOC/c) by Health Canada for the following indications: 1) as adjunctive treatment for the symptomatic relief of neuropathic pain in adult patients with multiple sclerosis; 2) as adjunctive analgesic treatment in adult patients with advanced cancer who experience moderate to severe pain during the highest tolerated dose of strong opioid therapy for persistent background pain [L886].
DB04871LorcaserinFor the treatment of obesity, as an adjunct to a reduced-calorie diet and increased physical activity.
DB12071VabicaserinNot Available
DrugDrug NameTargetType
DB00574Fenfluramine5-hydroxytryptamine receptor 2Ctarget
DB00574Fenfluramine5-hydroxytryptamine receptor 2Btarget
DB00574FenfluramineCytochrome P450 2D6enzyme
DB00574FenfluramineSodium-dependent serotonin transportertarget
DB00574Fenfluramine5-hydroxytryptamine receptor 2Atarget
DB01186PergolideDopamine D2 receptortarget
DB01186PergolideDopamine D1 receptortarget
DB01186PergolideDopamine D3 receptortarget
DB01186Pergolide5-hydroxytryptamine receptor 1Atarget
DB01186PergolideAlpha-1A adrenergic receptortarget
DB01186PergolideAlpha-2A adrenergic receptortarget
DB01186PergolideAlpha-2B adrenergic receptortarget
DB01186PergolideAlpha-2C adrenergic receptortarget
DB01186PergolideAlpha-1B adrenergic receptortarget
DB01186PergolideAlpha-1D adrenergic receptortarget
DB01186PergolideDopamine D4 receptortarget
DB01186PergolideDopamine D5 receptortarget
DB01186Pergolide5-hydroxytryptamine receptor 1Btarget
DB01186Pergolide5-hydroxytryptamine receptor 1Dtarget
DB01186Pergolide5-hydroxytryptamine receptor 2Atarget
DB01186Pergolide5-hydroxytryptamine receptor 2Btarget
DB01186Pergolide5-hydroxytryptamine receptor 2Ctarget
DB01186PergolideCytochrome P450 2D6enzyme
DB01186PergolideCytochrome P450 3A4enzyme
DB01200BromocriptineDopamine D2 receptortarget
DB01200BromocriptineCytochrome P450 3A4enzyme
DB01200Bromocriptine5-hydroxytryptamine receptor 1Dtarget
DB01200BromocriptineAlpha-2A adrenergic receptortarget
DB01200BromocriptineDopamine D3 receptortarget
DB01200Bromocriptine5-hydroxytryptamine receptor 1Atarget
DB01200BromocriptineAlpha-2C adrenergic receptortarget
DB01200BromocriptineAlpha-2B adrenergic receptortarget
DB01200Bromocriptine5-hydroxytryptamine receptor 2Btarget
DB01200BromocriptineDopamine D4 receptortarget
DB01200Bromocriptine5-hydroxytryptamine receptor 2Atarget
DB01200Bromocriptine5-hydroxytryptamine receptor 1Btarget
DB01200Bromocriptine5-hydroxytryptamine receptor 2Ctarget
DB01200BromocriptineDopamine D5 receptortarget
DB01200BromocriptineDopamine D1 receptortarget
DB01200BromocriptineAlpha-1A adrenergic receptortarget
DB01200BromocriptineAlpha-1B adrenergic receptortarget
DB01200BromocriptineAlpha-1D adrenergic receptortarget
DB01200Bromocriptine5-hydroxytryptamine receptor 7target
DB01200BromocriptineP-glycoprotein 1transporter
DB00248CabergolineDopamine D2 receptortarget
DB00248Cabergoline5-hydroxytryptamine receptor 2Btarget
DB00248CabergolineDopamine D3 receptortarget
DB00248Cabergoline5-hydroxytryptamine receptor 2Atarget
DB00248CabergolineAlpha-2B adrenergic receptortarget
DB00248Cabergoline5-hydroxytryptamine receptor 1Dtarget
DB00248CabergolineDopamine D4 receptortarget
DB00248CabergolineAlpha-2A adrenergic receptortarget
DB00248Cabergoline5-hydroxytryptamine receptor 1Atarget
DB00248CabergolineAlpha-2C adrenergic receptortarget
DB00248CabergolineDopamine D5 receptortarget
DB00248CabergolineDopamine D1 receptortarget
DB00248Cabergoline5-hydroxytryptamine receptor 1Btarget
DB00248Cabergoline5-hydroxytryptamine receptor 2Ctarget
DB00248CabergolineCytochrome P450 3A4enzyme
DB00248Cabergoline5-hydroxytryptamine receptor 7target
DB00248CabergolineAlpha-1A adrenergic receptortarget
DB00248CabergolineAlpha-1B adrenergic receptortarget
DB00248CabergolineAlpha-1D adrenergic receptortarget
DB00248CabergolineBeta-1 adrenergic receptortarget
DB00248CabergolineBeta-2 adrenergic receptortarget
DB00248CabergolineD(1) dopamine receptortarget
DB00248CabergolineP-glycoprotein 1transporter
DB00320Dihydroergotamine5-hydroxytryptamine receptor 1Dtarget
DB00320Dihydroergotamine5-hydroxytryptamine receptor 1Btarget
DB00320DihydroergotamineCytochrome P450 3A4enzyme
DB00320DihydroergotamineAlpha-2A adrenergic receptortarget
DB00320Dihydroergotamine5-hydroxytryptamine receptor 2Btarget
DB00320DihydroergotamineP-glycoprotein 1transporter
DB01454MidomafetamineSodium-dependent serotonin transportertarget
DB01454MidomafetamineSynaptic vesicular amine transportertarget
DB01454MidomafetamineSodium-dependent dopamine transportertarget
DB01454Midomafetamine5-hydroxytryptamine receptor 2Atarget
DB01454Midomafetamine5-hydroxytryptamine receptor 2Btarget
DB01454Midomafetamine5-hydroxytryptamine receptor 2Ctarget
DB01454MidomafetamineSodium-dependent noradrenaline transportertarget
DB01454MidomafetamineSodium-dependent noradrenaline transportertransporter
DB01454MidomafetamineSodium-dependent dopamine transportertransporter
DB01454MidomafetamineSodium-dependent serotonin transportertransporter
DB01454MidomafetamineCytochrome P450 2D6enzyme
DB04829Lysergic acid diethylamide5-hydroxytryptamine receptor 1Atarget
DB04829Lysergic acid diethylamide5-hydroxytryptamine receptor 2Btarget
DB04829Lysergic acid diethylamide5-hydroxytryptamine receptor 6target
DB04829Lysergic acid diethylamideCytochrome P450 3A4enzyme
DB04829Lysergic acid diethylamideCytochrome P450 2D6enzyme
DB00696ErgotamineAlpha-1A adrenergic receptortarget
DB00696Ergotamine5-hydroxytryptamine receptor 1Dtarget
DB00696Ergotamine5-hydroxytryptamine receptor 1Btarget
DB00696Ergotamine5-hydroxytryptamine receptor 2Atarget
DB00696ErgotamineAlpha-2A adrenergic receptortarget
DB00696ErgotamineDopamine D2 receptortarget
DB00696ErgotamineAlpha-2B adrenergic receptortarget
DB00696ErgotamineSodium-dependent noradrenaline transportertarget
DB00696ErgotamineCytochrome P450 3A4enzyme
DB00696ErgotamineAlpha-1B adrenergic receptortarget
DB00696ErgotamineAlpha-1D adrenergic receptortarget
DB00696ErgotamineP-glycoprotein 1transporter
DB00696ErgotamineD(1) dopamine receptortarget
DB00696Ergotamine5-hydroxytryptamine receptor 1Atarget
DB00696Ergotamine5-hydroxytryptamine receptor 1Ftarget
DB00696Ergotamine5-hydroxytryptamine receptor 2Ctarget
DB00696Ergotamine5-hydroxytryptamine receptor 2Btarget
DB01442MMDA5-hydroxytryptamine receptor 2Atarget
DB01442MMDASodium-dependent serotonin transportertarget
DB01442MMDASodium-dependent dopamine transportertarget
DB01442MMDAChromaffin granule amine transportertarget
DB01442MMDASynaptic vesicular amine transportertarget
DB01442MMDAAmine oxidase [flavin-containing] Atarget
DB01442MMDAAmine oxidase [flavin-containing] Btarget
DB01442MMDASodium-dependent noradrenaline transportertarget
DB139402,5-Dimethoxy-4-ethylthioamphetamine5-hydroxytryptamine receptor 2Atarget
DB139402,5-Dimethoxy-4-ethylthioamphetamine5-hydroxytryptamine receptor 2Ctarget
DB13948N-(2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine5-hydroxytryptamine receptor 2Atarget
DB140105-methoxy-N,N-dimethyltryptamine5-hydroxytryptamine receptor 1Atarget
DB140105-methoxy-N,N-dimethyltryptamine5-hydroxytryptamine receptor 2Atarget
DB140105-methoxy-N,N-dimethyltryptamineCytochrome P450 2D6enzyme
DB12110m-Chlorophenylpiperazine5-hydroxytryptamine receptor 2Ctarget
DB04948LofexidineAlpha-2A adrenergic receptortarget
DB04948LofexidineAlpha-1A adrenergic receptortarget
DB04948Lofexidine5-hydroxytryptamine receptor 1Atarget
DB04948Lofexidine5-hydroxytryptamine receptor 7target
DB04948Lofexidine5-hydroxytryptamine receptor 2Ctarget
DB04948Lofexidine5-hydroxytryptamine receptor 1Dtarget
DB04948LofexidineCytochrome P450 2D6enzyme
DB04948LofexidineCytochrome P450 1A2enzyme
DB04948LofexidineCytochrome P450 2C19enzyme
DB04948LofexidineATP-binding cassette sub-family B member 5transporter
DB04948LofexidineMultidrug and toxin extrusion protein 1transporter
DB09061CannabidiolCytochrome P450 2C9enzyme
DB09061CannabidiolCytochrome P450 2C19enzyme
DB09061CannabidiolCytochrome P450 2D6enzyme
DB09061CannabidiolCytochrome P450 3A4enzyme
DB09061CannabidiolCannabinoid receptor 1target
DB09061CannabidiolCannabinoid receptor 2target
DB09061CannabidiolG-protein coupled receptor 12target
DB09061CannabidiolGlycine receptor subunit alpha-1target
DB09061CannabidiolGlycine receptor (alpha-1/beta)target
DB09061CannabidiolGlycine receptor subunit alpha-3target
DB09061CannabidiolN-arachidonyl glycine receptortarget
DB09061CannabidiolG-protein coupled receptor 55target
DB09061Cannabidiol5-hydroxytryptamine receptor 1Atarget
DB09061Cannabidiol5-hydroxytryptamine receptor 2Atarget
DB09061CannabidiolNeuronal acetylcholine receptor subunit alpha-7target
DB09061CannabidiolDelta-type opioid receptortarget
DB09061CannabidiolMu-type opioid receptortarget
DB09061CannabidiolPeroxisome proliferator-activated receptor gammatarget
DB09061CannabidiolCytochrome P450 3A5enzyme
DB09061CannabidiolArylalkylamine N-acetyltransferaseenzyme
DB09061CannabidiolCytochrome P450 1A1enzyme
DB09061CannabidiolFatty-acid amide hydrolase 1enzyme
DB09061CannabidiolArachidonate 5-lipoxygenaseenzyme
DB09061CannabidiolArachidonate 15-lipoxygenaseenzyme
DB09061CannabidiolQuinone oxidoreductaseenzyme
DB09061CannabidiolMultidrug resistance-associated protein 1transporter
DB09061CannabidiolATP-binding cassette sub-family G member 2transporter
DB09061CannabidiolEquilibrative nucleoside transporter 1transporter
DB09061CannabidiolTransient receptor potential cation channel subfamily V member 1target
DB09061CannabidiolVoltage-dependent T-type calcium channel subunit alpha-1Gtarget
DB09061CannabidiolVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB09061CannabidiolVoltage-dependent T-type calcium channel subunit alpha-1Itarget
DB09061CannabidiolTransient receptor potential cation channel subfamily A member 1target
DB09061CannabidiolTransient receptor potential cation channel subfamily M member 8target
DB09061CannabidiolTransient receptor potential cation channel subfamily V member 2target
DB09061CannabidiolTransient receptor potential cation channel subfamily V member 3target
DB09061CannabidiolTransient receptor potential cation channel subfamily V member 4target
DB09061CannabidiolVoltage-dependent anion-selective channel protein 1target
DB09061Cannabidiol5-hydroxytryptamine receptor 3Atarget
DB09061CannabidiolAdenosine receptor A1target
DB09061CannabidiolProstaglandin G/H synthase 1target
DB09061CannabidiolProstaglandin G/H synthase 2target
DB09061CannabidiolAcetyl-CoA acetyltransferase, mitochondrialtarget
DB09061CannabidiolSteroid 17-alpha-hydroxylase/17,20 lyasetarget
DB09061Cannabidiol3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB09061CannabidiolGlutathione reductase, mitochondrialtarget
DB09061CannabidiolGlutathione peroxidase 1target
DB09061CannabidiolIndoleamine 2,3-dioxygenase 1target
DB09061CannabidiolCytochrome P450 1B1target
DB09061CannabidiolNAD(P)H dehydrogenase [quinone] 1target
DB09061CannabidiolCatalasetarget
DB09061CannabidiolCytochrome P450 3A5target
DB09061CannabidiolCytochrome P450 2D6target
DB09061CannabidiolSuperoxide dismutase [Cu-Zn]target
DB09061CannabidiolCytochrome P450 1A2target
DB09061CannabidiolCytochrome P450 3A7target
DB09061CannabidiolArylalkylamine N-acetyltransferasetarget
DB09061CannabidiolN-acylethanolamine-hydrolyzing acid amidasetarget
DB04871Lorcaserin5-hydroxytryptamine receptor 2Ctarget
DB04871LorcaserinCytochrome P450 1A2enzyme
DB04871LorcaserinCytochrome P450 2A6enzyme
DB04871LorcaserinCytochrome P450 2B6enzyme
DB04871LorcaserinCytochrome P450 2C19enzyme
DB04871LorcaserinCytochrome P450 2D6enzyme
DB04871LorcaserinCytochrome P450 3A4enzyme
DB04871LorcaserinDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB04871LorcaserinCytochrome P450 1A1enzyme