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ER |
Agonists |
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Steroidal: 2-Hydroxyestradiol
- 2-Hydroxyestrone
- 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
- 3α-Androstanediol
- 3α,5α-Dihydrolevonorgestrel
- 3β,5α-Dihydrolevonorgestrel
- 3α-Hydroxytibolone
- 3β-Hydroxytibolone
- 3β-Androstanediol
- 4-Androstenediol
- 4-Androstenedione
- 4-Fluoroestradiol
- 4-Hydroxyestradiol
- 4-Hydroxyestrone
- 4-Methoxyestradiol
- 4-Methoxyestrone
- 5-Androstenediol
- 7-Oxo-DHEA
- 7α-Hydroxy-DHEA
- 7α-Methylestradiol
- 7β-Hydroxyepiandrosterone
- 8,9-Dehydroestradiol
- 8,9-Dehydroestrone
- 8β-VE2
- 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED)
- 11β-Chloromethylestradiol
- 11β-Methoxyestradiol
- 15α-Hydroxyestradiol
- 16-Ketoestradiol
- 16-Ketoestrone
- 16α-Fluoroestradiol
- 16α-Hydroxy-DHEA
- 16α-Hydroxyestrone
- 16α-Iodoestradiol
- 16α-LE2
- 16β-Hydroxyestrone
- 16β,17α-Epiestriol (16β-hydroxy-17α-estradiol)
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17α-Estradiol (alfatradiol)
- 17α-Dihydroequilenin
- 17α-Dihydroequilin
- 17α-Epiestriol (16α-hydroxy-17α-estradiol)
- 17α-Ethynyl-3α-androstanediol
- 17α-Ethynyl-3β-androstanediol
- 17β-Dihydroequilenin
- 17β-Dihydroequilin
- 17β-Methyl-17α-dihydroequilenin
- Abiraterone
- Abiraterone acetate
- Alestramustine
- Almestrone
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Anabolic steroids (e.g., testosterone and esters, methyltestosterone, metandienone (methandrostenolone), nandrolone and esters, many others; via estrogenic metabolites)
- Atrimustine
- Bolandiol
- Bolandiol dipropionate
- Butolame
- Clomestrone
-
Cloxestradiol
- Conjugated estriol
- Conjugated estrogens
- Cyclodiol
- Cyclotriol
- DHEA
- DHEA-S
- ent-Estradiol
- Epiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol)
- Epimestrol
- Equilenin
- Equilin
- ERA-63 (ORG-37663)
- Esterified estrogens
- Estetrol
-
Estradiol
- Estramustine
- Estramustine phosphate
- Estrapronicate
- Estrazinol
-
Estriol
- Estrofurate
- Estrogenic substances
- Estromustine
-
Estrone
- Etamestrol (eptamestrol)
-
Ethinylandrostenediol
-
Ethinylestradiol
- Ethinylestriol
- Ethylestradiol
- Etynodiol
- Etynodiol diacetate
- Hexolame
- Hippulin
- Hydroxyestrone diacetate
- Lynestrenol
- Lynestrenol phenylpropionate
- Mestranol
- Methylestradiol
- Moxestrol
- Mytatrienediol
- Nilestriol
- Norethisterone
- Noretynodrel
- Orestrate
- Pentolame
- Prodiame
- Prolame
- Promestriene
- RU-16117
- Quinestradol
- Quinestrol
- Tibolone
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Xenoestrogens: Anise-related (e.g., anethole, anol, dianethole, dianol, photoanethole)
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Chalconoids (e.g., isoliquiritigenin, phloretin, phlorizin (phloridzin), wedelolactone)
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Coumestans (e.g., coumestrol, psoralidin)
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Flavonoids (incl. 7,8-DHF, 8-prenylnaringenin, apigenin, baicalein, baicalin, biochanin A, calycosin, catechin, daidzein, daidzin, ECG, EGCG, epicatechin, equol, formononetin, glabrene, glabridin, genistein, genistin, glycitein, kaempferol, liquiritigenin, mirificin, myricetin, naringenin, penduletin, pinocembrin, prunetin, puerarin, quercetin, tectoridin, tectorigenin)
- Lavender oil
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Lignans (e.g., enterodiol, enterolactone, nyasol (cis-hinokiresinol))
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Metalloestrogens (e.g., cadmium)
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Pesticides (e.g., alternariol, dieldrin, endosulfan, fenarimol, HPTE, methiocarb, methoxychlor, triclocarban, triclosan)
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Phytosteroids (e.g., digitoxin (digitalis), diosgenin, guggulsterone)
-
Phytosterols (e.g., β-sitosterol, campesterol, stigmasterol)
-
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol (teranol, β-zearalanol))
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Steroid-like (e.g., deoxymiroestrol, miroestrol)
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Stilbenoids (e.g., resveratrol, rhaponticin)
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Synthetic xenoestrogens (e.g., alkylphenols, bisphenols (e.g., BPA, BPF, BPS), DDT, parabens, PBBs, PHBA, phthalates, PCBs)
- Others (e.g., agnuside, rotundifuran)
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Mixed (SERMs) |
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Antagonists |
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Coregulator-binding modulators: ERX-11
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GPER |
Agonists |
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Antagonists |
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Unknown |
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Ionotropic |
GABAA |
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Positive modulators (abridged; see here for a full list): α-EMTBL
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Alcohols (e.g., drinking alcohol, 2M2B)
- Anabolic steroids
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Avermectins (e.g., ivermectin)
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Barbiturates (e.g., phenobarbital)
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Benzodiazepines (e.g., diazepam)
-
Bromide compounds (e.g., potassium bromide)
-
Carbamates (e.g., meprobamate)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
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Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
- Etazepine
- Etifoxine
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Fenamates (e.g., mefenamic acid)
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Flavonoids (e.g., apigenin, hispidulin)
- Fluoxetine
- Flupirtine
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Imidazoles (e.g., etomidate)
-
Kava constituents (e.g., kavain)
- Lanthanum
- Loreclezole
- Monastrol
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Neuroactive steroids (e.g., allopregnanolone, cholesterol, THDOC)
- Niacin
- Niacinamide
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Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
- Norfluoxetine
- Petrichloral
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Phenols (e.g., propofol)
- Phenytoin
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Piperidinediones (e.g., glutethimide)
- Propanidid
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Pyrazolopyridines (e.g., etazolate)
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Quinazolinones (e.g., methaqualone)
- Retigabine (ezogabine)
- ROD-188
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Skullcap constituents (e.g., baicalin)
- Stiripentol
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Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
- Topiramate
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Valerian constituents (e.g., valerenic acid)
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Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, sevoflurane)
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Negative modulators: 1,3M1B
- 3M2B
- 11-Ketoprogesterone
- 17-Phenylandrostenol
- α5IA (LS-193,268)
- β-CCB
- β-CCE
- β-CCM
- β-CCP
- β-EMGBL
- Anabolic steroids
- Amiloride
- Anisatin
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β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
- Basmisanil
- Bemegride
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Bicyclic phosphates (TBPS, TBPO, IPTBO)
- BIDN
- Bilobalide
- Bupropion
- CHEB
- Chlorophenylsilatrane
- Cicutoxin
- Cloflubicyne
- Cyclothiazide
- DHEA
- DHEA-S
- Dieldrin
- (+)-DMBB
- DMCM
- DMPC
- EBOB
- Etbicyphat
- FG-7142 (ZK-31906)
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Fiproles (e.g., fipronil)
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Flavonoids (e.g., amentoflavone, oroxylin A)
- Flumazenil
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Fluoroquinolones (e.g., ciprofloxacin)
- Flurothyl
- Furosemide
- Golexanolone
- Iomazenil (123I)
- IPTBO
- Isopregnanolone (sepranolone)
- L-655,708
- Laudanosine
- Leptazol
- Lindane
- MaxiPost
- Morphine
- Morphine-3-glucuronide
- MRK-016
- Naloxone
- Naltrexone
- Nicardipine
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Nonsteroidal antiandrogens (e.g., apalutamide, bicalutamide, enzalutamide, flutamide, nilutamide)
- Oenanthotoxin
- Pentylenetetrazol (pentetrazol)
- Phenylsilatrane
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Picrotoxin (i.e., picrotin, picrotoxinin and dihydropicrotoxinin)
- Pregnenolone sulfate
- Propybicyphat
- PWZ-029
- Radequinil
- Ro 15-4513
- Ro 19-4603
- RO4882224
- RO4938581
- Sarmazenil
- SCS
- Suritozole
- TB-21007
- TBOB
- TBPS
- TCS-1105
- Terbequinil
- TETS
- Thujone
- U-93631
- Zinc
- ZK-93426
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GABAA-ρ |
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Metabotropic |
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Angiopoietin |
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CNTF |
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EGF (ErbB) |
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FGF |
FGFR1 |
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FGFR2 |
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Agonists: Ersofermin
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FGF (1, 2 (bFGF), 3, 4, 5, 6, 7 (KGF), 8, 9, 10 (KGF2), 17, 18, 22)
- Palifermin
- Repifermin
- Selpercatinib
- Sprifermin
- Trafermin
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FGFR3 |
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FGFR4 |
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Unsorted |
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HGF (c-Met) |
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IGF |
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LNGF (p75NTR) |
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PDGF |
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RET (GFL) |
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SCF (c-Kit) |
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TGFβ |
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Trk |
TrkA |
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Negative allosteric modulators: VM-902A
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TrkB |
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Agonists: 3,7-DHF
- 3,7,8,2'-THF
- 4'-DMA-7,8-DHF
- 7,3'-DHF
- 7,8-DHF
- 7,8,2'-THF
- 7,8,3'-THF
- Amitriptyline
- BDNF
- BNN-20
- Deoxygedunin
- Deprenyl
- Diosmetin
- DMAQ-B1
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- R13
- TDP6
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TrkC |
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VEGF |
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Others |
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Additional growth factors: Adrenomedullin
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Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
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Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
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Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
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Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
-
Thrombopoietin (see here instead)
- Wnt signaling proteins
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Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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TRPA |
Activators |
- 4-Hydroxynonenal
- 4-Oxo-2-nonenal
- 4,5-EET
- 12S-HpETE
- 15-Deoxy-Δ12,14-prostaglandin J2
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α-Sanshool (ginger, Sichuan and melegueta peppers)
- Acrolein
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Allicin (garlic)
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Allyl isothiocyanate (mustard, radish, horseradish, wasabi)
- AM404
- ASP-7663
- Bradykinin
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Cannabichromene (cannabis)
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Cannabidiol (cannabis)
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Cannabigerol (cannabis)
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Cinnamaldehyde (cinnamon)
- CR gas (dibenzoxazepine; DBO)
- CS gas (2-chlorobenzal malononitrile)
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Cuminaldehyde (cumin)
-
Curcumin (turmeric)
-
Dehydroligustilide (celery)
- Diallyl disulfide
-
Dicentrine (Lindera spp.)
- Farnesyl thiosalicylic acid
- Formalin
-
Gingerols (ginger)
- Hepoxilin A3
- Hepoxilin B3
- Hydrogen peroxide
- Icilin
- Isothiocyanate
- JT-010
-
Ligustilide (celery, Angelica acutiloba)
-
Linalool (Sichuan pepper, thyme)
- Methylglyoxal
-
Methyl salicylate (wintergreen)
- N-Methylmaleimide
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Nicotine (tobacco)
-
Oleocanthal (olive oil)
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Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- PF-4840154
- Phenacyl chloride
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Polygodial (Dorrigo pepper)
-
Shogaols (ginger, Sichuan and melegueta peppers)
- Tear gases
-
Tetrahydrocannabinol (cannabis)
- Tetrahydrocannabiorcol
-
Thiopropanal S-oxide (onion)
-
Umbellulone (Umbellularia californica)
- WIN 55,212-2
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Blockers |
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TRPC |
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TRPM |
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TRPML |
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TRPP |
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TRPV |
Activators |
- 2-APB
- 5',6'-EET
- 9-HODE
- 9-oxoODE
- 12S-HETE
- 12S-HpETE
- 13-HODE
- 13-oxoODE
- 20-HETE
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α-Sanshool (ginger, Sichuan and melegueta peppers)
-
Allicin (garlic)
- AM404
- Anandamide
-
Bisandrographolide (Andrographis paniculata)
-
Camphor (camphor laurel, rosemary, camphorweed, African blue basil, camphor basil)
-
Cannabidiol (cannabis)
-
Cannabidivarin (cannabis)
-
Capsaicin (chili pepper)
-
Carvacrol (oregano, thyme, pepperwort, wild bergamot, others)
- DHEA
- Diacyl glycerol
-
Dihydrocapsaicin (chili pepper)
- Estradiol
-
Eugenol (basil, clove)
-
Evodiamine (Euodia ruticarpa)
-
Gingerols (ginger)
- GSK1016790A
- Heat
- Hepoxilin A3
- Hepoxilin B3
-
Homocapsaicin (chili pepper)
-
Homodihydrocapsaicin (chili pepper)
-
Incensole (incense)
- Lysophosphatidic acid
- Low pH (acidic conditions)
-
Menthol (mint)
- N-Arachidonoyl dopamine
- N-Oleoyldopamine
- N-Oleoylethanolamide
-
Nonivamide (PAVA) (PAVA spray)
-
Nordihydrocapsaicin (chili pepper)
-
Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- Phenylacetylrinvanil
-
Phorbol esters (e.g., 4α-PDD)
-
Piperine (black pepper, long pepper)
-
Polygodial (Dorrigo pepper)
- Probenecid
- Protons
- RhTx
-
Rutamarin (Ruta graveolens)
-
Resiniferatoxin (RTX) (Euphorbia resinifera/pooissonii)
-
Shogaols (ginger, Sichuan and melegueta peppers)
-
Tetrahydrocannabivarin (cannabis)
-
Thymol (thyme, oregano)
-
Tinyatoxin (Euphorbia resinifera/pooissonii)
- Tramadol
-
Vanillin (vanilla)
- Zucapsaicin
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Blockers |
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