SR 58611A (hydrochloride)

SR 58611A is a selective beta3-adrenergic receptor agonist (beta3-AR, EC50 = 3.5 nM in rat colon). Its activity cannot be blocked by the beta1- and beta2-AR antagonists CGP 20712A and ICI 118551 (Cay-15591), respectively. SR 58611A is minimally active against beta1-ARs in rat uterus (EC50 = 499 nM) and inactive against beta2-ARs in guinea pig trachea and atrium (EC50s = >10,000 and >30,000 nM, respectively). SR 58611A activates brown fat metabolism through activation of adenylyl cyclase activity and glycerol release in brown adipocytes (EC50s = 20 and 11 nM, respectively). It also reduces hypothermia produced by apomorphine (Cay-16094) and reserpine (Cay-16474) and potentiates toxicity produced by yohimbine (Cay-19869) in mice. SR 58611A (0.6 to 2 mg/kg/day) also reduces the number of escape failures in a learned helplessness model of antidepressant-like activity in rats without changes in locomotor activity typically seen with beta2-AR agonists.Formal Name: [[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]oxy]-acetic acid, ethyl ester, monohydrochloride. CAS Number: 121524-09-2. Synonyms: Amibegron. Molecular Formula: C22H26ClNO4 . HCl. Formula Weight: 440.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 277 nm. SMILES: CCOC(COC1=CC=C(CC[C@H](NC[C@H](O)C2=CC(Cl)=CC=C2)C3)C3=C1)=O.Cl. InChi Code: InChI=1S/C22H26ClNO4.ClH/c1-2-27-22(26)14-28-20-9-7-15-6-8-19(11-17(15)12-20)24-13-21(25)16-4-3-5-18(23)10-16,/h3-5,7,9-10,12,19,21,24-25H,2,6,8,11,13-14H2,1H3,1H/t19-,21-,/m0./s1. InChi Key: NQIZCDQCNYCVAS-RQBPZYBGSA-N.