195875-84-4
195875-84-4 structure
- Name: Tesofensine
- Chemical Name: (1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8- azabicyclo[3.2.1]octane
- CAS Number: 195875-84-4
- Molecular Formula: C17H23Cl2NO
- Molecular Weight: 328.27700
- Catalog: Signaling Pathways Neuronal Signaling Dopamine Transporter
- Create Date: 2016-02-13 20:56:45
- Modify Date: 2025-08-25 08:31:14
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Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent[1]. Tesofensine is a CNS acting anti-obesity agent[2].
| Name | (1R,2R,3S,5S)-3-(3,4-Dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8- azabicyclo[3.2.1]octane |
|---|---|
| Synonyms | Tesofensine |
| Description | Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent[1]. Tesofensine is a CNS acting anti-obesity agent[2]. |
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| Related Catalog | |
| Target |
DA/NE/5-HT[1] |
| In Vivo | Tesofensine (a single dose of 0.1-3 mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3 mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12 h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0 mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls[3]. Animal Model: Diet-induced obesity (DIO) rat[3] Dosage: 0.1-3 mg/kg Administration: Administered subcutaneously (s.c.); a single dose (acute treatment) Result: The threshold dose for inhibition of total food intake was 1.0 mg/kg. The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3 mg/kg. Animal Model: Diet-induced obesity (DIO) rat[3] Dosage: 2.0 mg/kg Administration: Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment) Result: The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%. When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%. |
| References |
| Density | 1.161 g/cm3 |
|---|---|
| Boiling Point | 396.6ºC at 760 mmHg |
| Molecular Formula | C17H23Cl2NO |
| Molecular Weight | 328.27700 |
| Flash Point | 193.7ºC |
| Exact Mass | 327.11600 |
| PSA | 12.47000 |
| LogP | 4.53410 |