CP-809101 hydrochloride

SKU: orb1940804

Description

CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist (pEC50: 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors).(In Vitro):CP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro.(In Vivo):Similar to currently available antipsychotic drugs, CP-809101 dose-dependently inhibited conditioned avoidance responding (CAR, ED50 = 4.8 mg/kg, sc). CP-809101 antagonized both PCP- and d-amphetamine-induced hyperactivity with ED50 values of 2.4 and 2.9 mg/kg (sc), respectively, and also reversed an apomorphine induced-deficit in prepulse inhibition. At doses up to 56 mg/kg, CP-809101 did not produce catalepsy. CP-809101 was inactive in two animal models of antidepressant-like activity, the forced swim test, and learned helplessness.

Key Properties

• CAS Number: 1215721-40-6
• MW: 341.24
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₈Cl₂N₄O
• SMILES: Cl.Clc1cccc(COc2cncc(n2)N2CCNCC2)c1
• Target: 5-HT Receptor
• Solubility: In Vitro: H2O : 20 mg/mL (58.61 mM)

Bioactivity

• In Vivo:
  CP-809101 hydrochloride (0.1-56 mg/kg; s. c. ; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner. CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s. c. ; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner). CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s. c. ; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg. CP-809101 hydrochloride (0.3, 1, 3 mg/kg; s. c. ; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine. Animal model: Male CF rats (conditioned avoidance responding (CAR) model). Dosage: 0.1-56 mg/kg. Administration: Subcutaneous injection; single. Result: Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg. Animal model: Male CD rats (PCP or d-amphetamine-induced hyperactivity model). Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg. Administration: Subcutaneous injection; single. Result: Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg. Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner. Animal model: Male CD rats (spontaneous locomotor model). Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg. Administration: Subcutaneous injection; single. Result: Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50 = 2.7 mg/kg). Animal model: Adult male Sprague-Dawley rats (280-400 g). Dosage: 0.3, 1, 3 mg/kg. Administration: Subcutaneous injection; single. Result: Produced a dose-related decrease in responding for food and nicotine self-administration in rats.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

5-HT Receptor