2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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CP94253

CP94253 Chemical Structure

CAS No. : 131084-35-0

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Description

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[1][2][3][4][5][6].

IC50 & Target

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)

In Vitro

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 Related Antibodies
In Vivo

CP94253 (1-10 mg/kg; i.p.; single dose) dose-dependently reduces food intake in female Wistar rats with an ED50 of 3.48 mg/kg i.p. for the first hour of access, its hypophagic effect is not mediated by 5-HT2C receptors, and it has its hypophagic action potentiated by pretreatment with a low, inactive dose of the 5-HT2C agonist ORG 37684 (HY-103120)[1].
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.

Animal Model: Wistar (female, ~200 g body weight)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Albino Swiss (male, 24-26 g)[2]
Dosage: 5 mg/kg
Administration: i.p.; single dose
Result: Shortened the immobility time of mice by 43%.
Did not alter spontaneous locomotor activity of mice.
Animal Model: Wistar (male, 350-380 g, implanted with chronic sleep recording electrodes, habituated to recording chambers and injection procedures)[3]
Dosage: 0.5 mg/kg; 1.0 mg/kg; 5.0 mg/kg; 10.0 mg/kg
Administration: s.c.
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.
Animal Model: Wistar (male, 350-380 g, implanted with chronic sleep recording electrodes, pretreated with (±) Pindolol)[3]
Dosage: 5.0 mg/kg plus 2.0 mg/kg (±) Pindolol; 10.0 mg/kg plus 2.0 mg/kg (±) Pindolol
Administration: s.c.
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.
Animal Model: Charles River Sprague-Dawley CD (male, 170-190 g)[4]
Dosage: 3.2 mg/kg; 10 mg/kg; 32 mg/kg
Administration: p.o.; daily; 9 days
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.
Animal Model: CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
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
Administration: i.p.; single dose
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.
Animal Model: CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
Dosage: 3.0 mg/kg; 5.6 mg/kg; 10.0 mg/kg
Administration: i.p.; single dose
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.
Animal Model: CFW (male, adult, 20-25 g, arrived at 5 weeks old)[5]
Dosage: 1.0 mg/kg; 3.0 mg/kg; 10.0 mg/kg
Administration: i.p.; single dose
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.
Animal Model: Sprague-Dawley (male, mildly food-deprived)[6]
Dosage: 5 µmol/kg; 10 µmol/kg; 14 µmol/kg; 20 µmol/kg; 40 µmol/kg
Administration: i.p.; single injection 30 minutes prior to feeding
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.
Animal Model: Sprague-Dawley (male, mildly food-deprived)[6]
Dosage: 5 µmol/kg; 10 µmol/kg; 14 µmol/kg; 20 µmol/kg; 40 µmol/kg
Administration: i.p.; single injection 30 minutes prior to sucrose access
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.
Molecular Weight

257.33

Formula

C15H19N3O
CAS No.
SMILES

CCCOC1=NC2=C(NC=C2C3=CCNCC3)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CP94253131084-35-0CP 94253CP-942535-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorWistar ratsCFW micenoradrenaline systems5-HT1B receptordopamine systemsdepressionforced swimming testrodents5-HT2C receptorrat cerebral cortex membraneInhibitorinhibitorinhibit

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