SR 58611A (hydrochloride)
SR 58611A is a selective ?3-adrenergic receptor agonist (?3-AR; EC50 = 3.5 nM in rat colon).{38085} Its activity cannot be blocked by the ?1- and ?2-AR antagonists CGP 20712A and ICI 118551 (Item No. 15591), respectively. SR 58611A is minimally active against ?1-ARs in rat uterus (EC50 = 499 nM) and inactive against ?2-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).{38086} It also reduces hypothermia produced by apomorphine (Item No. 16094) and reserpine (Item No. 16474) and potentiates toxicity produced by yohimbine (Item No. 19869) in mice.{38087} 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 ?2-AR agonists.
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