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Fig. 1 · Structure
Cat. No.
A10674
CAS No.
99614-01-4
Formula
C18H19N3O.HCl
Mol. Weight
329.82

Documents & Downloads

Ondansetron HCl (GR 38032F)

Cat. No. A10674 CAS 99614-01-4

5-HT Receptors antagonist

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy.

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Biological Activity

Target & Activity

Target Activity Value
5-HT3

In Vitro Studies

Ondansetron treatment increased thermogenic gene mRNA expression in immortalized brown adipocytes compared with vehicle. Expression was assessed by quantitative reverse transcriptase–PCR. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Ondansetron and thermogenic gene expression in brown adipocytes

Cell-based study · immortalized brown adipocytes (IBA); n=4 per group [1]

In immortalized brown adipocytes, ondansetron treatment increased thermogenic gene mRNA expression compared with vehicle, as assessed by quantitative reverse transcriptase–PCR.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Expression of thermogenesis-related genes in IBA was assessed by quantitative reverse transcriptase–PCR (qRT–PCR)Reported result After 2 h ondansetron (1 μM) treatment: Ondansetron also increased the mRNA expression of thermogenic genes, such as Ucp1 and Ppargc1a, in IBA; *P<0.05 and **P<0.01 versus vehicle.[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 μM
Exposure duration
2 h
Method
treatment
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Ondansetron

The paper names Ondansetron without stating the salt or form; not verified as the hydrochloride form supplied as A10674. No dose conversion or lot validation.

Results > 5-HT regulates thermogenesis via Htr3 (S65, S69); Figure 9 legend (S240)

Expression of thermogenesis-related genes in IBA was assessed by quantitative reverse transcriptase–PCR (qRT–PCR): Expression of thermogenesis-related genes in IBA was assessed by quantitative reverse transcriptase–PCR (qRT–PCR); comparator: vehicle — Results > 5-HT regulates thermogenesis via Htr3 (S69); Figure 9 legend (S240)

In Vivo Studies

In BALB/c mice, intraperitoneal Ondansetron was not effective in reducing cisplatin-induced body weight loss when comparing cisplatin at MTD with or without Ondansetron. In sham Sprague Dawley rats, topical spinal application of Ondansetron did not produce significant inhibition of low threshold evoked responses compared with pre-drug baseline control data. Topical spinal application of Ondansetron significantly inhibited the heat-evoked neuronal response in sham Sprague Dawley rats compared with pre-drug baseline control data. [2,3]

Ondansetron and cisplatin-induced weight loss in mice

Animal study · BALB/c mice [2]

In BALB/c mice, intraperitoneal ondansetron was evaluated by comparing cisplatin at MTD with or without ondansetron. Ondansetron was not effective in reducing cisplatin-induced body weight loss.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Individual maximum body weight loss as compared to starting weightReported result Ondansetron was not effective in reducing weight loss induced by cisplatin; ondansetron was dosed at the commonly reported dose of 1 mg/kg in mice; dosed on the day of chemotherapy administration and for 3 days post chemotherapy.[2]

Conditions shared by the study groups

Route
intraperitoneally (i.p)
Treatment course
on the day of chemotherapy administration and for 3 days post chemotherapy
Vehicle
sterile water for injection
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ondansetron 1 mg/kgcisplatin at MTD with or without ondansetronOndansetron was not effective in reducing weight loss induced by cisplatin; ondansetron was dosed at the commonly reported dose of 1 mg/kg in mice; dosed on the day of chemotherapy administration and for 3 days post chemotherapy.[2]
Ondansetron 1 mg/kg
Model: BALB/c mice
Methods and source locations

Compound reported in the paper: Ondansetron

The paper names Ondansetron without stating the salt or form; not verified as the hydrochloride form supplied as A10674. No dose conversion or lot validation.

Methods > Chemotherapy dosing (S8); Methods > Effect of supportive care on chemotherapy-induced weight-loss (S21, S22, S23); Results > Determination of MTD of selected chemotherapeutics (S28); Results > Effect of supportive care on chemotherapy-induced weight loss (S59, S63)

Individual maximum body weight loss as compared to starting weight: Individual maximum body weight loss as compared to starting weight; comparator: cisplatin at MTD with or without ondansetron — Methods > Effect of supportive care on chemotherapy-induced weight-loss (S22, S23); Results > Effect of supportive care on chemotherapy-induced weight loss (S59, S63)

Ondansetron 1 mg/kg · Methods > Chemotherapy dosing (S8); Methods > Effect of supportive care on chemotherapy-induced weight-loss (S22, S23); Results > Effect of supportive care on chemotherapy-induced weight loss (S59)

Ondansetron and low threshold evoked responses in rats

Animal study · Sprague Dawley rats; sham (n = 8) [3]

In sham Sprague Dawley rats, ondansetron administered by topical spinal application did not produce significant inhibition of low threshold evoked responses compared with pre-drug baseline control data.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
low threshold evoked responsesReported result 10, 50 and 100 μg/50 μl: ondansetron did not produce any significant inhibition of these low threshold evoked responses in the control group.[3]

Conditions shared by the study groups

Route
topical spinal application with a Hamilton syringe
Treatment course
tests carried out at 20, 40 and 60 minutes before subsequent drug applications
Vehicle
0.9% saline solution
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ondansetron 10, 50 and 100 μg/50 μlpre- drug baseline control data10, 50 and 100 μg/50 μl: ondansetron did not produce any significant inhibition of these low threshold evoked responses in the control group.[3]
Ondansetron 10, 50 and 100 μg/50 μl
Model: Sprague Dawley rats; sham (n = 8)
Methods and source locations

Compound reported in the paper: Ondansetron

The paper names Ondansetron without stating the salt or form; not verified as the hydrochloride form supplied as A10674. No dose conversion or lot validation.

Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S17, S18); Methods > Induction of Osteoarthritis (S37); Methods > Electrophysiology (S51); Methods > Drug administration (S66, S68); Figure 3 legend (S92, S94)

low threshold evoked responses: low threshold evoked responses; comparator: pre- drug baseline control data — Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S18); Methods > Drug administration (S66)

Ondansetron 10, 50 and 100 μg/50 μl · Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S18); Methods > Drug administration (S66, S68)

Ondansetron and heat-evoked neuronal responses in rats

Animal study · Sprague Dawley rats; sham (n = 8) [3]

Ondansetron at 10 μg produced a significant inhibition of the evoked neuronal response to 40°C in the sham control group.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
evoked neuronal response to 40°CReported result Ondansetron at 10 μg produced a significant inhibition of the evoked neuronal response to 40°C in the sham control group[3]

Conditions shared by the study groups

Route
topical spinal application with a Hamilton syringe
Treatment course
tests carried out at 20, 40 and 60 minutes before subsequent drug applications
Vehicle
0.9% saline solution
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ondansetron 10 μgpre- drug baseline control dataOndansetron at 10 μg produced a significant inhibition of the evoked neuronal response to 40°C in the sham control group[3]
Ondansetron 10 μg
Model: Sprague Dawley rats; sham (n = 8)
Methods and source locations

Compound reported in the paper: Ondansetron

The paper names Ondansetron without stating the salt or form; not verified as the hydrochloride form supplied as A10674. No dose conversion or lot validation.

Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S21); Methods > Induction of Osteoarthritis (S37); Methods > Electrophysiology (S51, S58); Methods > Drug administration (S66, S68); Figure 3 legend (S94); Figure 4 legend (S95, S96, S97)

evoked neuronal response to 40°C: evoked neuronal response to 40°C; comparator: pre- drug baseline control data — Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S21)

Ondansetron 10 μg · Results > Effects of spinal ondansetron administration on the evoked responses of dorsal horn neurones (S21); Methods > Drug administration (S66, S68)

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 99614-01-4
Applications 5-HT Receptors antagonist
Formula C18H19N3O.HCl
Molecular Weight 329.82
Synonyms Ondemet; Emeset; Emetron; GR 38032F
SMILES
CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 59 mg/mL (178.88 mM)
Water 22 mg/mL (66.7 mM)
Ethanol 9 mg/mL (27.28 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Oh CM, Namkung J, Go Y, et al. Regulation of systemic energy homeostasis by serotonin in adipose tissues. Nat Commun (2015). PMID: 25864946 DOI: 10.1038/ncomms7794 Source material
  2. [2] Aston WJ, Hope DE, Nowak AK, et al. A systematic investigation of the maximum tolerated dose of cytotoxic chemotherapy with and without supportive care in mice. BMC Cancer (2017). PMID: 29037232 DOI: 10.1186/s12885-017-3677-7 Source material
  3. [3] Rahman W, Bauer CS, Bannister K, et al. Descending serotonergic facilitation and the antinociceptive effects of pregabalin in a rat model of osteoarthritic pain. Mol Pain (2009). PMID: 19664204 DOI: 10.1186/1744-8069-5-45 Source material

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