Product Name

Sibutramine Hydrochloride

CAS Number

84485-00-7

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Product Name:
Sibutramine Hydrochloride
CAS Number:
84485-00-7
Indication:
For the treatment of obesity.
Mode of Action:

Sibutramine produces its therapeutic effects by inhibition of norepinephrine (NE), serotonin (5-hydroxytryptamine, 5-HT), and to a lesser extent, dopamine reuptake at the neuronal synapse. By inhibiting the reuptake of these neurotransmitters, sibutramine promotes a sense of satiety and decrease in appetite, thereby reducing food intake. Data from animal studies also suggest that sibutramine may also increase energy expenditure through thermogenic effects in both the basal and fed states, but this has not been confirmed in humans. Sibutramine and its major pharmacologically active metabolites (M1 and M2) do not act via release of monoamines.

Pharmacodynamics:

Sibutramine is an orally administered agent for the treatment of obesity. Sibutramine exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin and norepinephrine reuptake in vivo, but not in vitro. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vitro and in vivo. In human brain tissue, M1 and M2 also inhibit dopamine reuptake in vitro, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Sibutramine, M1 and M2 exhibit no evidence of anticholinergic or antihistaminergic actions. In addition, receptor binding profiles show that sibutramine, M1 and M2 have low affinity for serotonin (5-HT1, 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C), norepinephrine (b, b1, b3, a1 and a2), dopamine (D1 and D2), benzodiazepine, and glutamate (NMDA) receptors. These compounds also lack monoamine oxidase inhibitory activity in vitro and in vivo.

Metabolism:

Hepatic

Toxicity:

Side effects include dry mouth, anorexia, insomnia, constipation and headache.

IUPAC:
Cyclobutanemethanamine, 1-(4-chlorophenyl)-N, N-dimethyl-alpha-(2-methylpropyl)-, hydrochloride
ATC:
A08AA10
PubChem:
5210
DrugBank:
DB01105
Formula:
C17-H26-Cl-N.Cl-H
Molecular Mass:
316.3133
Synonyms:
1-(4-Chlorophenyl)-N,N-dimethyl-alpha-(2-methylpropyl)cyclobutanemethanamine hydrochloride, BTS 54524, Meridia, Reductil, Sibutramine HCl, UNII-9GG866ZP1E, Yeduc
SMILES:
CC(C)CC(C1(CCC1)c2ccc(cc2)Cl)N(C)C.Cl
AHFS Code:
28:20.9
InChi:
1S/C17H26ClN.ClH/c1-13(2)12-16(19(3)4)17(10-5-11-17)14-6-8-15(18)9-7-14;/h6-9,13,16H,5,10-12H2,1-4H3;1H
General Reference:
General Reference:

  1. Sharma B, Henderson DC: Sibutramine: current status as an anti-obesity drug and its future perspectives. Expert Opin Pharmacother. 2008 Aug;9(12):2161-73. Pubmed
  2. Tziomalos K, Krassas GE, Tzotzas T: The use of sibutramine in the management of obesity and related disorders: an update. Vasc Health Risk Manag. 2009;5(1):441-52. Pubmed
  3. Heal DJ, Aspley S, Prow MR, Jackson HC, Martin KF, Cheetham SC: Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord. 1998 Aug;22 Suppl 1:S18-28; discussion S29. Pubmed
  4. Stock MJ: Sibutramine: a review of the pharmacology of a novel anti-obesity agent. Int J Obes Relat Metab Disord. 1997 Mar;21 Suppl 1:S25-9. Pubmed

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