CP94253
CP94253 is an orally active, brain-penetrant and selective 5-HT1B receptor agonist with an Ki of 2 nM. CP94253 induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 can be used for the research of depression and heightened aggressive behavior.
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- No. CAS: 131084-35-0
- Fòrmula: C15H19N3O
- Peso molecular:257.33
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Actividad biológica
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5-HT1B Receptor 2 nM (Ki) |
5-HT1D Receptor 49 nM (Ki) |
5-HT1A Receptor 89 nM (Ki) |
5-HT1C Receptor 860 nM (Ki) |
5-HT2 Receptor 1600 nM (Ki) |
CP94253 potently and selectively binds to 5-HT1B receptors (Ki = 2 nM) with minimal affinity for other serotonin receptor subtypes and no significant binding to a broad range of off-target receptors[3].
CP94253 (1.0-2.0 nM) acts as a competitive inhibitor of [125I]iodocyanopindolol binding to rat cerebral cortex membrane 5-HT1B receptors[4].
CP94253 (50-100 nM) competitively inhibits [3H]5-HT binding to bovine caudate membrane 5-HT1D receptors[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CP94253 (5 mg/kg; i.p.; single dose) exerts a potent antidepressant-like effect in mice, reducing forced swimming test immobility time by 43%, via stimulation of 5-HT1B receptors (likely postsynaptic or heteroreceptors), with dopamine and noradrenaline systems contributing to this action[2].
CP94253 (0.5-10.0 mg/kg; s.c.) activates 5-HT1B receptors with dose-dependently increasing waking and reducing SWS (at 5.0-10.0 mg/kg) and suppresses REMS across all tested doses in male Wistar rats[3].
CP94253 (5.0-10.0 mg/kg; s.c.)-induced increases in waking and reductions in SWS can be reversed by pretreatment with 2.0 mg/kg (±) Pindolol (HY-B0982)[3].
CP94253 (3.2-32 mg/kg; p.o.; daily; 9 days) administered orally to healthy rats induces transient anorexia, sustained reduced body weight gain, and persistent hyperlocomotion at 32 mg/kg, while 3.2 mg/kg and 10 mg/kg doses show no significant effects on these endpoints[4].
CP94253 (3-17 mg/kg; i.p.; single dose) dose-dependently reduces species-typical aggression in male CFW mice with an ED50 of 7.2 mg/kg for attack bite reduction, an effect specific to 5-HT1B receptors as shown by antagonism with GR 127935 (HY-123869) and no effect of WAY 100,635 (HY-10349), without concurrent locomotor sedation[5].
CP94253 (3-10 mg/kg; i.p.; single dose) reduces alcohol-heightened aggression in male CFW mice with a lower ED50 (3.8 mg/kg) than for non-heightened aggression, with dose-dependent effects that only reduce locomotor behaviors at the highest tested dose[5].
CP94253 (1-10 mg/kg; i.p.; single dose) reduces instigation-heightened aggression in male CFW mice with a lower ED50 (2.7 mg/kg) than for non-instigated aggression, with dose-dependent effects on locomotor behaviors only at higher doses[5].
CP94253 (5-40 µmol/kg; i.p.; single injection 30 minutes prior to feeding) produces a potent hypophagic effect in mildly deprived rats consuming pellets, with an ID50 of 12.5 µmol/kg, by reducing meal duration and feeding frequency without altering resting behaviour[6].
CP94253 (5-28 µmol/kg; i.p.; single injection 30 minutes prior to sucrose access) produces a hypophagic effect in mildly deprived rats consuming 10% sucrose, with an ID50 of 22.8 µmol/kg, by reducing meal duration, feeding frequency, and licking burst/cluster frequency without impairing oral motor efficiency[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (female, ~200 g body weight)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Induced a dose-dependent reduction of food intake, with an ED50 value of 3.48 mg/kg for the first hour of food access.
Showed hypophagic effect unaffected by pretreatment with 5-HT2C receptor antagonists metergoline or SB 242,084.
Had hypophagic effect potentiated by pretreatment with a low, inactive dose of ORG 37684, lowering its ED50 to 2.44 mg/kg for the 0-1 h interval, 1.19 mg/kg for the 0-2 h interval, and 1.93 mg/kg for the 0-6 h interval.
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Animal Model:Albino Swiss (male, 24-26 g)[2]
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Dosage:5 mg/kg
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Administration:i.p.; single dose
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Result:Shortened the immobility time of mice by 43%.
Did not alter spontaneous locomotor activity of mice.
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Animal Model:Wistar (male, 350-380 g, implanted with chronic sleep recording electrodes, habituated to recording chambers and injection procedures)[3]
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Dosage:0.5 mg/kg; 1.0 mg/kg; 5.0 mg/kg; 10.0 mg/kg
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Administration:s.c.
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Result:Decreased REM sleep to 8.8 minutes and number of REM periods to 3.5 during 0-3 hour period at 0.5 mg/kg; no significant changes to waking, slow wave sleep, or light sleep observed at 0.5 mg/kg.
Decreased REM sleep to 4.3 minutes and number of REM periods to 2.0, and increased REM sleep latency to 90.8 minutes during 0-3 hour period at 1.0 mg/kg; decreased REM sleep to 11.0 minutes and number of REM periods to 4.1 during 4-6 hour period at 1.0 mg/kg.
Increased waking to 86.0 minutes, decreased slow wave sleep to 71.9 minutes and REM sleep to 1.4 minutes, increased REM sleep latency to 164.6 minutes, and decreased number of REM periods to 0.7 during 0-3 hour period at 5.0 mg/kg; increased waking to 58.4 minutes, decreased slow wave sleep to 92.6 minutes and REM sleep to 4.7 minutes, and decreased number of REM periods to 2.3 during 4-6 hour period at 5.0 mg/kg.
Increased waking to 96.9 minutes and light sleep to 34.5 minutes, decreased slow wave sleep to 48.3 minutes and REM sleep to 0.3 minutes, increased slow wave sleep latency to 23.4 minutes and REM sleep latency to 239.2 minutes, and decreased number of REM periods to 0.2 during 0-3 hour period at 10.0 mg/kg; increased waking to 79.9 minutes and light sleep to 36.8 minutes, decreased slow wave sleep to 59.1 minutes and REM sleep to 4.2 minutes, and decreased number of REM periods to 2.0 during 4-6 hour period at 10.0 mg/kg.
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Animal Model:Wistar (male, 350-380 g, implanted with chronic sleep recording electrodes, pretreated with (±) Pindolol)[3]
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Dosage:5.0 mg/kg plus 2.0 mg/kg (±) Pindolol; 10.0 mg/kg plus 2.0 mg/kg (±) Pindolol
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Administration:s.c.
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Result:Decreased REM sleep to 2.9 minutes and number of REM periods to 1.6, and increased REM sleep latency to 125.0 minutes during 0-3 hour period at 5.0 mg/kg with (±) Pindolol pretreatment.
Decreased REM sleep to 6.0 minutes and number of REM periods to 2.9 during 4-6 hour period at 5.0 mg/kg with (±) Pindolol pretreatment.
No significant changes to waking or slow wave sleep observed at 5.0 mg/kg with (±) Pindolol pretreatment.
Decreased REM sleep to 2.7 minutes and number of REM periods to 1.6, and increased REM sleep latency to 135.6 minutes during 0-3 hour period at 10.0 mg/kg with (±) Pindolol pretreatment.
Decreased REM sleep to 3.4 minutes and number of REM periods to 3.1 during 4-6 hour period at 10.0 mg/kg with (±) Pindolol pretreatment.
No significant changes to waking or slow wave sleep observed at 10.0 mg/kg with (±) Pindolol pretreatment.
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Animal Model:Charles River Sprague-Dawley CD (male, 170-190 g)[4]
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Dosage:3.2 mg/kg; 10 mg/kg; 32 mg/kg
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Administration:p.o.; daily; 9 days
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Result:Reduced attack bite and tail rattle frequencies significantly at all tested doses (3-17 mg/kg).
Reduced sideways threats significantly at 10.0 and 17.0 mg/kg.
Achieved an ED50 of 7.2 mg/kg for attack bite reduction.
Shifted the ED50 for attack bite reduction to 14.5 mg/kg when pretreated with GR 127935.
Shifted the ED50 for sideways threat reduction to 15.6 mg/kg when pretreated with GR 127935.
Did not alter anti-aggressive effects when pretreated with WAY 100,635.
Did not reduce locomotor behaviors (walking, rearing) at any tested dose.
Decreased grooming duration at all doses.
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Animal Model:CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
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Dosage:3.0 mg/kg; 5.6 mg/kg; 10.0 mg/kg; 17.0 mg/kg; 10 mg/kg plus GR 127935; 17 mg/kg plus GR 127935; 30 mg/kg plus GR 127935
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Administration:i.p.; single dose
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Result:Reduced attack bite and tail rattle frequencies significantly at all tested doses (3-17 mg/kg).
Reduced sideways threats significantly at 10.0 and 17.0 mg/kg.
Achieved an ED50 of 7.2 mg/kg for attack bite reduction.
Shifted the ED50 for attack bite reduction to 14.5 mg/kg when pretreated with GR 127935.
Shifted the ED50 for sideways threat reduction to 15.6 mg/kg when pretreated with GR 127935.
Did not alter anti-aggressive effects when pretreated with WAY 100,635.
Did not reduce locomotor behaviors (walking, rearing) at any tested dose.
Decreased grooming duration at all doses.
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Animal Model:CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
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Dosage:3.0 mg/kg; 5.6 mg/kg; 10.0 mg/kg
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Administration:i.p.; single dose
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Result:Reduced attack bite and sideways threat frequencies significantly at all tested doses (3-10 mg/kg).
Reduced tail rattle frequency at 10.0 mg/kg.
Achieved an ED50 of 3.8 mg/kg for attack bite reduction in alcohol-heightened aggression mice, which was significantly lower than the ED50 of 7.1 mg/kg in alcohol-non-heightened aggression mice.
Reduced locomotor behaviors (walking, rearing) only at the 10.0 mg/kg dose.
Did not significantly affect grooming duration.
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Animal Model:CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
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Dosage:1.0 mg/kg; 3.0 mg/kg; 10.0 mg/kg
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Administration:i.p.; single dose
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Result:Reduced attack bite and sideways threat frequencies significantly at 3.0 and 10.0 mg/kg.
Achieved an ED50 of 2.7 mg/kg for attack bite reduction in instigation-heightened aggression mice, which was significantly lower than the ED50 of 8.3 mg/kg for non-instigated aggression.
Reduced walking duration at 3.0 and 10.0 mg/kg.
Reduced rearing and grooming durations only at 10.0 mg/kg.
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Animal Model:Sprague-Dawley (male, mildly food-deprived)[6]
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Dosage:5 µmol/kg; 10 µmol/kg; 14 µmol/kg; 20 µmol/kg; 40 µmol/kg
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Administration:i.p.; single injection 30 minutes prior to feeding
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Result:Produced a dose-related decrease in 30-minute pellet intake, with significant reductions at 10, 14, 20, and 40 µmol/kg.
Reduced water intake in a non-systematic, non-dose-related manner across all doses.
Reduced the frequency of feeding observations at all doses.
Shortened meal duration in a dose-related manner.
Increased standing at the 20 µmol/kg dose.
Left resting frequency unchanged.
Induced an abnormal prone posture at the 40 µmol/kg dose.
Achieved an ID50 of 12.5 µmol/kg for pellet intake reduction.
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Animal Model:Sprague-Dawley (male, mildly food-deprived)[6]
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Dosage:5 µmol/kg; 10 µmol/kg; 14 µmol/kg; 20 µmol/kg; 40 µmol/kg
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Administration:i.p.; single injection 30 minutes prior to sucrose access
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Result:Produced a dose-related decrease in 30-minute sucrose intake, with significant reductions at 20 and 28 µmol/kg.
Reduced the frequency of feeding observations at 20 and 28 µmol/kg.
Shortened meal duration in a dose-related manner.
Increased standing at the 28 µmol/kg dose.
Left resting frequency unchanged.
Reduced the total number of licks at 20 and 28 µmol/kg, with lick efficiency unchanged.
Decreased the frequency of licking bursts and clusters without altering their size.
Achieved an ID50 of 22.8 µmol/kg for sucrose intake reduction.
Chemical Information
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No. CAS 131084-35-0
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Peso molecular 257.33
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Fòrmula C15H19N3O
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SMILES
CCCOC1=NC2=C(NC=C2C3=CCNCC3)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Schreiber R, et al. Role of 5-hT2C receptors in the hypophagic effect of m-CPP, ORG 37684 and CP-94,253 in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2002;26(3):441-449. [Content Brief]
[2]. Tatarczyńska E, et al. Antidepressant-like effect of the selective 5-HT1B receptor agonist CP 94253: a possible mechanism of action. Eur J Pharmacol. 2005;516(1):46-50. [Content Brief]
[3]. Monti JM, et al. Effects of selective activation of the 5-HT1B receptor with CP-94,253 on sleep and wakefulness in the rat. Neuropharmacology. 1995 Dec;34(12):1647-51. [Content Brief]
[5]. Fish EW, et al. Aggression heightened by alcohol or social instigation in mice: reduction by the 5-HT(1B) receptor agonist CP-94,253. Psychopharmacology (Berl). 1999;146(4):391-399. [Content Brief]
[6]. Lee MD, et al. CP-94, 253: a selective serotonin1B (5-HT1B) agonist that promotes satiety. Psychopharmacology (Berl). 1997;131(3):264-270. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP94253 Related Classifications
HY-103151A Related Classifications
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