Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C10H14ClN.ClH |
| Molecular Weight | 220.139 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(C)(N)CC1=CC=C(Cl)C=C1
InChI
InChIKey=WEJDYJKJPUPMLH-UHFFFAOYSA-N
InChI=1S/C10H14ClN.ClH/c1-10(2,12)7-8-3-5-9(11)6-4-8;/h3-6H,7,12H2,1-2H3;1H
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/13931448 | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2274216/pdf/canfamphys00340-0041.pdf
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/13931448 | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2274216/pdf/canfamphys00340-0041.pdf
Chlorphentermine exerts anorectic properties. It is a synthetic amphetamine derivatc claimed to have none of the excitatory effects of the parenit substanice. PRE-SATE (Chlorphentermine HCl) is an effective appetite suppressant with a pattern of pharmacologic action substantially different from those of traditional anorexigenics. In providing dependable appetite control with appreciable loss of bodyweight, PRE-SATE does not significantly increase central nervous system (CNS), cardiorespiratory or metabolic activity.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL228 |
338.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | PRE-SATE Approved UsePRE-SATE is indicated as an adlunct in the short term (i.e. a few weeks) management of exogenous obesity and related less serious overweight conditions in conjunction with a medically supervised regimen of weight reduction based on caloric restriction. |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5416167/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
CHLORPHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
10.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5416167/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
CHLORPHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
41 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5416167/ |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
CHLORPHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Chlorphentermine, a new anorectic agent. | 1962 Sep |
|
| Experimental myopathy induced by amphiphilic cationic compounds including several psychotropic drugs. | 1979 |
|
| The early changes in experimental myopathy induced by chloroquine and chlorphentermine. | 1980 Jan |
|
| The effect of fenfluramine on the pulmonary disposition of 5-hydroxytryptamine in the isolated perfused rat lung: a comparison with chlorphentermine. | 2000 Jan |
|
| Anorexigen-induced pulmonary hypertension and the serotonin (5-HT) hypothesis: lessons for the future in pathogenesis. | 2002 |
|
| The use of parotid gland activity analysis in patients with gastro-esophageal reflux disease (GERD) and bulimia nervosa. | 2006 |
|
| Screening for amphetamine and amphetamine-type drugs in doping analysis by liquid chromatography/mass spectrometry. | 2006 |
|
| The antidotal effects of high-dosage gamma-aminobutyric acid on acute tetramine poisoning as compared with sodium dimercaptopropane sulfonate. | 2007 Aug |
|
| Gene expression in lungs of mice lacking the 5-hydroxytryptamine transporter gene. | 2009 May 10 |
|
| Successful drug development despite adverse preclinical findings part 2: examples. | 2010 Dec |
|
| Pulmonary hypertension associated with use of phentermine. | 2010 Nov |
|
| Insight into human alveolar macrophage and M. tuberculosis interactions via metabolic reconstructions. | 2010 Oct 19 |
Patents
Sample Use Guides
Adults: 65 mg (one tablet) taken with or shortly after the first meal of the day.
Route of Administration:
Oral
In contrast, lymphocytes pre-incubated with 10(-5)M chlorphentermine (CP) for 60 min, then stimulated with Con A for 2 hours in the presence of 10(-5)M CP, exhibit a significantly depressed inositol phosphate formation. In addition, CP also inhibited the activity of phospholipase C (IC50 = 0.58 mM), the enzyme responsible for the formation of inositol phosphates during lymphocyte activation. Further, lymphocytes activated in a manner that bypasses the phosphatidylinositol pathway are not inhibited by 10(-7)M or 10(-9)M CP as are cells activated with Con A.
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NCI_THESAURUS |
C47795
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DEA NO. |
1645
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RL11HOJ7DM
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76098
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DTXSID1047815
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C65324
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205-782-9
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m3458
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65477
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CHEMBL1201269
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100000084738
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DBSALT000815
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SUB01251MIG
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151-06-4
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ACTIVE MOIETY
SUBSTANCE RECORD
