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

CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT1B receptor agonist with an Ki of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior.

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CP94253 hydrochloride

CP94253 hydrochloride Chemical Structure

CAS No. : 845861-39-4

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Based on 1 publication(s) in Google Scholar

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CP94253 hydrochloride Related Antibodies

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Description

CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT1B receptor agonist with an Ki of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior[1][2][3][4][5][6].

IC50 & Target[3]

5-HT1B Receptor

2 nM (Ki)

5-HT1A Receptor

89 nM (Ki)

5-HT1D Receptor

49 nM (Ki)

5-HT2A Receptor

1600 nM (Ki)

5-HT2C Receptor

860 nM (Ki)

In Vitro

CP94253 hydrochloride 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) hydrochloride acts as a competitive inhibitor of [125I]iodocyanopindolol binding to rat cerebral cortex membrane 5-HT1B receptors[4].
CP94253 (50-100 nM) hydrochloride 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 hydrochloride Related Antibodies
In Vivo

CP94253 (1-10 mg/kg; i.p.; single dose) hydrochloride 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) hydrochloride 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.) hydrochloride 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.) hydrochloride-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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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 food intake significantly in the first 24 hours (to ~14 g/24 hr, compared to vehicle ~24 g/24 hr), with the anorectic effect diminishing over time and returning to vehicle levels by day 7.
Inhibited body weight gain after the first and second injections, with a persistent weight differential relative to vehicle-treated rats maintained for the entire study (day 9 body weight ~290 g, compared to vehicle ~320 g).
Induced a ~2-fold increase in horizontal locomotion relative to vehicle starting on day 1, which persisted throughout the 9-day study with slight evidence of tolerance.
Showed no significant effect on food intake or body weight gain relative to vehicle at 3.2 mg/kg and 10 mg/kg.
Exerted little or no effect on horizontal locomotion at 3.2 mg/kg and 10 mg/kg.
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

293.79

Formula

C15H20ClN3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCCOC1=CC=C(NC=C2C3=CCNCC3)C2=N1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (425.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4038 mL 17.0190 mL 34.0379 mL
5 mM 0.6808 mL 3.4038 mL 6.8076 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4038 mL 17.0190 mL 34.0379 mL 85.0948 mL
5 mM 0.6808 mL 3.4038 mL 6.8076 mL 17.0190 mL
10 mM 0.3404 mL 1.7019 mL 3.4038 mL 8.5095 mL
15 mM 0.2269 mL 1.1346 mL 2.2692 mL 5.6730 mL
20 mM 0.1702 mL 0.8509 mL 1.7019 mL 4.2547 mL
25 mM 0.1362 mL 0.6808 mL 1.3615 mL 3.4038 mL
30 mM 0.1135 mL 0.5673 mL 1.1346 mL 2.8365 mL
40 mM 0.0851 mL 0.4255 mL 0.8509 mL 2.1274 mL
50 mM 0.0681 mL 0.3404 mL 0.6808 mL 1.7019 mL
60 mM 0.0567 mL 0.2836 mL 0.5673 mL 1.4182 mL
80 mM 0.0425 mL 0.2127 mL 0.4255 mL 1.0637 mL
100 mM 0.0340 mL 0.1702 mL 0.3404 mL 0.8509 mL
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  • Do most proteins show cross-species activity?

    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:

CP94253845861-39-4CP 94253CP-942535-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorWistar ratsCFW micenoradrenaline systems5-HT1B receptordopamine systemsdepressionforced swimming testrodents5-HT2C receptorrat cerebral cortex membraneInhibitorinhibitorinhibit

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