ADX71441 Names IUPAC name N -[5-[4-[(4-chloro-3-fluorophenyl)methyl]-6-methoxy-3,5-dioxo-1,2,4-triazin-2-yl]-2-fluorophenyl]acetamide
Identifiers Key: BQDMEJYNGXEHSW-UHFFFAOYSA-N
InChI=1S/C19H15ClF2N4O4/c1-10(27)23-16-8-12(4-6-14(16)21)26-19(29)25(18(28)17(24-26)30-2)9-11-3-5-13(20)15(22)7-11/h3-8H,9H2,1-2H3,(H,23,27)
CC(=O)NC1=C(C=CC(=C1)N2C(=O)N(C(=O)C(=N2)OC)CC3=CC(=C(C=C3)Cl)F)F
Properties C 19 H 15 Cl F 2 N 4 O 4 Molar mass −1 Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Infobox references
ADX-71441 is a GABAB receptor positive allosteric modulator currently being investigated as a potential treatment for anxiety, epilepsy, pain and other conditions.
Therapeutic potential
Addiction ADX-71441 has been shown to reduce alcohol consumption .[ 1] [ 2] [ 3]
There were also trials about nicotine addiction , which showed positive results: ADX-71441 was able to decrease some withdrawal symptoms of nicotine withdrawal .[ 4]
Anxiety This compound has also been shown to reduce anxiety in people with PTSD .[ 5]
Pain Experiments have shown that this compound was able to decrease hypersensitivity to pain in mice, Guinea pigs and rats.[ 5]
Tolerance ADX-71441 has been shown to have less tolerance and side effects than direct GABAB agonists, such as baclofen .[ 2]
References ^ "Addex Reports ADX71441 Reduces Alcohol Intake in a Preclinical Model of Chronic Alcohol Dependence" . Addex therapeutics . Retrieved 2024-02-03 .^ a b Augier E, Dulman RS, Damadzic R, Pilling A, Hamilton JP, Heilig M (August 2017). "The GABAB Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats" . Neuropsychopharmacology . 42 (9): 1789– 1799. doi :10.1038/npp.2017.53 . PMC 5520784 PMID 28294133 . ^ Colombo G (March 2024). "Positive allosteric modulators of the GABAB receptor: a new class of ligands with therapeutic potential for alcohol use disorder". Alcohol and Alcoholism . 59 (3). Oxford, Oxfordshire. doi :10.1093/alcalc/agae018 . PMID 38566580 . ^ "Addex ADX71441 Positive Results in Preclinical Model of Nicotine Addiction" . Addex therapeutics . Retrieved 2024-02-03 .^ a b Kalinichev M, Girard F, Haddouk H, Rouillier M, Riguet E, Royer-Urios I, et al. (March 2017). "The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity". Neuropharmacology . 114 : 34– 47. doi :10.1016/j.neuropharm.2016.11.016 . PMID 27889489 . S2CID 36606154 .
Ionotropic
GABAA Tooltip γ-Aminobutyric acid A receptor Positive modulators (abridged; see here for a full list): α-EMTBLAlcohols (e.g., drinking alcohol , 2M2B )Anabolic steroids Avermectins (e.g., ivermectin )Barbiturates (e.g., phenobarbital )Benzodiazepines (e.g., diazepam )Bromide compounds (e.g., potassium bromide )Carbamates (e.g., meprobamate )Carbamazepine Chloralose Chlormezanone Clomethiazole Dihydroergolines (e.g., ergoloid (dihydroergotoxine) )Etazepine Etifoxine Fenamates (e.g., mefenamic acid )Flavonoids (e.g., apigenin , hispidulin )Fluoxetine Flupirtine Imidazoles (e.g., etomidate )Kava constituents (e.g., kavain )Lanthanum Loreclezole Monastrol Neuroactive steroids (e.g., allopregnanolone , cholesterol , THDOC )Niacin Niacinamide Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil ), cyclopyrrolones (e.g., zopiclone ), imidazopyridines (e.g., zolpidem ), pyrazolopyrimidines (e.g., zaleplon ))Norfluoxetine Petrichloral Phenols (e.g., propofol )Phenytoin Piperidinediones (e.g., glutethimide )Propanidid Pyrazolopyridines (e.g., etazolate )Quinazolinones (e.g., methaqualone )Retigabine (ezogabine) ROD-188 Skullcap constituents (e.g., baicalin )Stiripentol Sulfonylalkanes (e.g., sulfonmethane (sulfonal) ) Topiramate Valerian constituents (e.g., valerenic acid )Volatiles /gases (e.g., chloral hydrate , chloroform , diethyl ether , paraldehyde , sevoflurane )Negative modulators: 1,3M1B3M2B 11-Ketoprogesterone 17-Phenylandrostenol α3IA α5IA (LS-193,268) β-CCB β-CCE β-CCM β-CCP β-EMGBL Anabolic steroids Amiloride Anisatin β-Lactams (e.g., penicillins , cephalosporins , carbapenems )Basmisanil Bemegride 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) Fiproles (e.g., fipronil ) Flavonoids (e.g., amentoflavone , oroxylin A )Flumazenil Fluoroquinolones (e.g., ciprofloxacin )Flurothyl Furosemide Golexanolone Iomazenil (123 I) IPTBO Isopregnanolone (sepranolone) L-655,708 Laudanosine Lindane MaxiPost Morphine Morphine-3-glucuronide MRK-016 Naloxone Naltrexone Nicardipine Nonsteroidal antiandrogens (e.g., apalutamide , bicalutamide , enzalutamide , flutamide , nilutamide )Oenanthotoxin Pentylenetetrazol (pentetrazol) Phenylsilatrane 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 GABAA -ρ Tooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABAB Tooltip γ-Aminobutyric acid B receptor Negative modulators: Compound 14
See also Receptor/signaling modulators GABAA receptor positive modulators GABA metabolism/transport modulators
