Chlorphentermine
Phentermine
Aminorex, fenfluramine, and chlorphentermine are serotonin transporter substrates. Implications for primary pulmonary hypertension. (1/6)
BACKGROUND: Coadministration of phentermine and fenfluramine (phen/fen) effectively treats obesity and possibly addictive disorders. The association of fenfluramine and certain other anorexic agents with serious side effects, such as cardiac valvulopathy and primary pulmonary hypertension (PPH), limits the clinical utility of these drugs. Development of new medications that produce neurochemical effects like phen/fen without causing unwanted side effects would be a significant therapeutic breakthrough. METHODS AND RESULTS: We tested the hypothesis that fenfluramine (and other anorexic agents) might increase the risk of PPH through interactions with serotonin (5-HT) transporters. Because 5-HT transporter proteins in the lung and brain are identical, we examined, in rat brain, the effects of selected drugs on 5-HT efflux in vivo and monoamine transporters in vitro as a generalized index of transporter function. Our data show that drugs known or suspected to increase the risk of PPH (eg, aminorex, fenfluramine, and chlorphentermine) are 5-HT transporter substrates, whereas drugs that have not been shown to increase the risk of PPH are less potent in this regard. CONCLUSIONS: We speculate that medications that are 5-HT transporter substrates get translocated into pulmonary cells where, depending on the degree of drug retention, their intrinsic drug toxicity, and individual susceptibility, PPH could develop as a response to high levels of these drugs or metabolites. Emerging evidence suggests that it is possible to develop transporter substrates devoid of adverse side effects. Such medications could have therapeutic application in the management of obesity, drug dependence, depression, and other disorders. (+info)The metabolism, distribution and elimination of chlorphentermine in man. (2/6)
1 A gas-liquid chromatography procedure for the determination of chlorphentermine (I), N-hydroxychlorphentermine (II) and alpha,alpha-dimethyl-alpha-nitro-beta-(4-chlorophenyl)ethane (IV) in urine has been developed. Also methods are reported to determine conjugated II and the total N-oxidized metabolites of I, i.e. II, conjugated II, alpha,alpha-dimethyl-alpha-nitroso-beta-(4-chlorophenyl)ethane (III) and IV in urine. 2 The synthesis of alpha,alpha-dimethyl-alpha-nitroso-beta-(4-chlorophenyl)ethane (III) and its properties are reported. 3 The kinetics of urinary excretion of I and its metabolic products after the oral administration of I to a human subject on separate occasions have been studied. Under normal conditions of urinary pH, metabolism by N-oxidation was the main elimination route of I; acidifying the urine increased the urinary excretion of unchanged I at the expense of the N-oxidized products. 4 The importance of the N-oxidation metabolic route in the distribution of chlorphentermine (I) in man is discussed. (+info)N-[11C-Methyl]chlorphentermine and N,N-[11C-dimethyl]chlorphentermine as brain blood-flow agents for positron emission tomography. (3/6)
N-[11C-methyl]chlorphentermine ([11C]NMCP) and N,N-[11C-dimethyl]chlorphentermine ([11C]NDMCP) were prepared from chlorphentermine and 11CH3I in DMF and evaluated in rats as brain blood-flow agents for positron emission tomography (PET). Tissue distribution of [11C]NMCP showed that brain uptake was 2.70 +/- 0.40% of injected dose per organ at 5 min with no change in radioactivity concentration up to 30 min after i.v. injection. Approximately 80% of the initial brain uptake remained at 60 min. On the other hand, initial brain uptake of [11C] NDMCP (3.66 +/- 0.31 and 3.63 +/- 0.88% injected dose per organ at 5 and 15 min, respectively) was greater than that of [11C]NMCP. The brain activity however, rapidly decreased to 2.38 +/- 0.17 and 1.82 +/- 0.32% at 30 and 60 min, respectively. Because of its longer retention in the brain compared with [11C]NDMCP, [11C]NMCP would be a potential brain blood-flow agent for quantitative PET studies. (+info)Fluorescence studies of the binding of amphiphilic amines with phospholipids. (4/6)
The binding characteristics of several amine drugs with dispersed phospholipids (phosphatidylcholine, phosphatidylserine, and phosphatidylglycerol) have been studied using the fluorometric method and 1-anilino-8-naphthalene sulfonate and 1,6 diphenyl-1,3,5-hexatriene as fluorescence probes. The results show that amphiphilic amines, such as chlorphentermine, interact with phospholipids via both ionic and hydrophobic forces. The ionic interaction, which occurs between the protonated amine group of the drug and the phosphate oxygen of the lipid, changes the amphiphilic characteristics of the lipid by reducing the number of negative charges on the lipid vesicles, and inhibits the Ca2+-dependent lipid hydrolysis by blocking the Ca2+ binding sites on the lipid vesicles. The hydrophobic interaction, which involves the nonpolar moieties of the drug and the lipid, is of primary importance to the overall drug-lipid binding stability. Drugs without a strong hydrophobic moiety, such as dopamine, do not interact with phospholipids. (+info)Comparative potencies of amphetamine, fenfluramine and related compounds in taste aversion experiments in rats. (5/6)
1 Rats failed to drink a flavoured solution when its consumption had been followed by injection of amphetamine (conditioned taste aversion).2 There was very little difference between the potencies of (+)- and (-)-amphetamine.3p-Chloromethamphetamine was a more potent aversive agent than methamphetamine.4 Strong taste aversions were also conditioned with other congeners of amphetamine. The rank order of potency was: fenfluramine > chlorphentermine >p-hydroxyamphetamine.5 Cocaine induced only moderate taste aversions, even at high doses.6 Aversive potency did not appear to be correlated with known neurochemical actions of the drugs or with behavioural stimulation, but appeared to be a central action which may have been linked to anorexigenic potency or time course of action. (+info)Effect of chlorphentermine on the lipids of rat lungs. (6/6)
Chronic administration of chlorphentermine to rats resulted in a reduction of body weight compared to a normal control group. The weight of the heart, liver, kidney, and spleen was less in the treated group while the weight of the lungs was increased significantly. There was no change in the ratio of right ventricular to left ventricular weight in the rats treated with chlorphentermine, supporting the views that this drug does not cause pulmonary hypertension. Biochemical analysis showed that the increase in the weight of the lungs was due to the accumulation of phospholipid. All classes of phospholipid were affected, but particularly phosphatidyl choline, the tissue concentration of which increased nine times. Chlorphentermine also increased the proportion of palmitate present in pulmonary phosphatidyl choline. Histological examination of the lung after treatment with chlorphentermine showed evidence of this drug-induced lipidosis. No conclusion can as yet be reached as to the mechanism involved in the accumulation of phospholipid in the lung after chlorphentermine. (+info)
Chlorphentermine - Wikipedia
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Chlorphentermine
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Chlorphentermine
... acts as a highly selective serotonin releasing agent (SRA). It is not a psychostimulant and has little or no ... Chlorphentermine (trade names Apsedon, Desopimon, Lucofen) is a serotonergic appetite suppressant of the amphetamine family. ... Rothman RB, Ayestas MA, Dersch CM, Baumann MH (August 1999). "Aminorex, fenfluramine, and chlorphentermine are serotonin ... "Chlorphentermine, a new anorectic agent". The Journal of Pharmacology and Experimental Therapeutics. 137: 365-73. PMID 13903304 ...
Cloforex
It is a prodrug to chlorphentermine. It never became a mass produced drug in part due to the side effects found in mice. Mice ... and reversal of pulmonary lipid histiocytosis in rats following oral administration of anorectics cloforex and chlorphentermine ...
Etolorex
Made by the reaction of chlorphentermine with 2-Chloroethanol. 3,4-Dichloroamphetamine Cericlamine Chlorphentermine Cloforex ...
Serotonin releasing agent
Chlorphentermine (Apsedon, Desopimon, Lucofen) Cloforex (Oberex) (prodrug of chlorphentermine) Dexfenfluramine (Redux) ( ... Fenfluramine, chlorphentermine, and aminorex, which are also amphetamines and relatives, were formerly used as appetite ... related to chlorphentermine; never marketed) Indeloxazine (Elen, Noin) (non-selective; discontinued) Levofenfluramine ( ... enantiomer of fenfluramine) Etolorex (prodrug of chlorphentermine; never marketed) Fenfluramine (Pondimin, Fen-Phen) Flucetorex ...
3,4-Methylenedioxyphentermine
3,4-Dichloroamphetamine Cericlamine Chlorphentermine Cloforex Clortermine Etolorex Phentermine MDPH entry in PiHKAL "UK Misuse ...
Clortermine
... produces very low rates of self-administration in animals similarly to chlorphentermine, and as a result it likely ... 4-Dichloroamphetamine Cericlamine Chlorphentermine Cloforex Etolorex Methylenedioxyphentermine Phentermine US patent 3415937, " ... and is the 2-chloro positional isomer of chlorphentermine. ...
2-Nitropropane
... chlorphentermine, and teclozan. It serves as an oxidant in the Hass-Bender oxidation process. 2-Nitropropane is a constituent ...
3,4-Dichloroamphetamine
3-Methoxy-4-methylamphetamine Cericlamine Chlorphentermine Clortermine Etolorex 3,4-Methylenedioxyamphetamine ...
5-HT2B receptor
MDMA MDA MEM Pergolide Cabergoline Norfenfluramine Chlorphentermine Aminorex Bromo-dragonfly DMT 5-MeO-DMT LSD - About equal ...
Controlled Drugs and Substances Act
Chlorphentermine (1-(p-chlorophenyl)-2-methyl-2-aminopropane) and any salt thereof Diethylpropion (2-(diethylamino) ...
List of drugs: Cf-Ch
... chlorphentermine (INN) chlorproethazine (INN) chlorproguanil (INN) chlorpromazine (INN) chlorpropamide (INN) chlorprothixene ( ...
Misuse of Drugs Act (Singapore)
Amobarbital Aprobarbital Benzphetamine Butabarbital Chlorphentermine Diazepam (valium) Flunitrazepam (rohypnol) Flutoprazepam ( ...
Serotonin
... chlorphentermine, and aminorex), and certain anti-Parkinsonian dopaminergic agonists, which also stimulate serotonergic 5-HT2B ...
Cardiac fibrosis
The drugs most classically associated with the condition are weight loss drugs such as fenfluramine and chlorphentermine, and ... chlorphentermine, and aminorex (along with its analogue 4-Methylaminorex which has seen sporadic use as a recreational drug) ...
C10H14ClN
... para-Chloromethamphetamine 3-Chloromethamphetamine 4-Chlorophenylisobutylamine Chlorphentermine Clortermine N,N-Dimethyl-2- ...
Cericlamine
3,4-Dichloroamphetamine Alaproclate Bupropion Chlorphentermine Clortermine Cloforex Etolorex Femoxetine Ifoxetine Indalpine ... and closely related to chlorphentermine, a highly selective serotonin releasing agent) that was investigated as an ...
List of MeSH codes (D02)
... chlorphentermine MeSH D02.092.471.683.152.766.617 - mephentermine MeSH D02.092.471.683.221 - butoxamine MeSH D02.092.471.683. ...
Misuse of Drugs Act 1977
Chlorphentermine Diethylpropion Ethchlorvnol (presumably Ethchlorvynol) Ethinamate Flunitrazepam (moved up from Schedule 4 by ...
Para-Chloroamphetamine
Substituted amphetamines para-Chloromethamphetamine (4-CMA) Chlorphentermine 3,4-Dichloroamphetamine (DCA) 4-Fluoroamphetamine ...
Chlorphentermine: Uses, Interactions, Mechanism of Action | DrugBank Online
Chlorphentermine. Clinical Trials. Clinical Trials Phase. Status. Purpose. Conditions. Count. Pharmacoeconomics. Manufacturers ... Chlorphentermine hydrochloride. RL11HOJ7DM. 151-06-4. WEJDYJKJPUPMLH-UHFFFAOYSA-N. International/Other Brands. Apsedon / ... Chlorphentermine may decrease the sedative and stimulatory activities of Acrivastine.. Adenosine. The risk or severity of ... Chlorphentermine. DrugBank Accession Number. DB01556. Background. A sympathomimetic agent that was formerly used as an ...
Lisdexamfetamine - Wikipedia
The oral bioavailability of amphetamine varies with gastrointestinal pH;[58] it is well absorbed from the gut, and bioavailability is typically over 75% for dextroamphetamine.[81] Amphetamine is a weak base with a pKa of 9.9;[82] consequently, when the pH is basic, more of the drug is in its lipid soluble free base form, and more is absorbed through the lipid-rich cell membranes of the gut epithelium.[82][58] Conversely, an acidic pH means the drug is predominantly in a water-soluble cationic (salt) form, and less is absorbed.[82] Approximately 20% of amphetamine circulating in the bloodstream is bound to plasma proteins.[5] Following absorption, amphetamine readily distributes into most tissues in the body, with high concentrations occurring in cerebrospinal fluid and brain tissue.[83] The half-lives of amphetamine enantiomers differ and vary with urine pH.[82] At normal urine pH, the half-lives of dextroamphetamine and levoamphetamine are 9-11 hours and 11-14 hours, respectively.[82] Highly ...
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NIOSHTIC-2 Publications Search - 00181128 - Biochemical characteristics of rat alveolar macrophages with chlorphentermine...
... in alveolar macrophages from male Long-Evans-hooded-rats treated 5 days a week for 4 weeks with chlorphentermine, 30mg/kg ... Experiments were described using centrifugal elutriation to study chlorphentermine (461789) induced phospholipidosis ... Experiments were described using centrifugal elutriation to study chlorphentermine (461789) induced phospholipidosis in ... Biochemical characteristics of rat alveolar macrophages with chlorphentermine-induced phospholipidosis: variations with ...
Amoxicillin - Wikipedia
Adverse effects are similar to those for other β-lactam antibiotics, including nausea, vomiting, rashes, and antibiotic-associated colitis. Loose bowel movements (diarrhea) may also occur. Rarer adverse effects include mental changes, lightheadedness, insomnia, confusion, anxiety, sensitivity to lights and sounds, and unclear thinking. Immediate medical care is required upon the first signs of these adverse effects.[citation needed] The onset of an allergic reaction to amoxicillin can be very sudden and intense; emergency medical attention must be sought as quickly as possible. The initial phase of such a reaction often starts with a change in mental state, skin rash with intense itching (often beginning in fingertips and around groin area and rapidly spreading), and sensations of fever, nausea, and vomiting. Any other symptoms that seem even remotely suspicious must be taken very seriously. However, more mild allergy symptoms, such as a rash, can occur at any time during treatment, even up to ...
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Phentermine AND Human[MH] AND (drug induced liver injury OR jaundice/CI OR bile duct diseases/CI OR liver/DE OR liver diseases...
Metabolism and distribution of chlorphentermine and clorofex in animal and man]. Bülow M, Dell HD, Fiedler J, Kamp R, Lorenz D. ... Whereas 20 mg/kg chlorphentermine for 7 days failed to markedly alter the incorporation of thymidine into kidney and liver DNA ... Whereas 20 mg/kg chlorphentermine for 7 days failed to markedly alter the incorporation of thymidine into kidney and liver DNA ... Renal and hepatic nucleic acid metabolism in neonates: relation to experimental duration, chlorphentermine dose as well as ...
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MeSH Browser
Chlorphentermine Hydrochloride Narrower Concept UI. M0004195. Registry Number. RL11HOJ7DM. Terms. Chlorphentermine ... Chlorphentermine Preferred Term Term UI T007954. Date01/01/1999. LexicalTag NON. ThesaurusID ... Chlorphentermine Preferred Concept UI. M0004194. Registry Number. NHW07912O7. Related Numbers. 151-06-4. 461-78-9. RL11HOJ7DM. ... Chlorphentermine Hydrochloride Desopimon Pre-Sate Pharm Action. Sympathomimetics. Registry Number. NHW07912O7. Related Numbers ...
MeSH Browser
Chlorphentermine Hydrochloride Narrower Concept UI. M0004195. Registry Number. RL11HOJ7DM. Terms. Chlorphentermine ... Chlorphentermine Preferred Term Term UI T007954. Date01/01/1999. LexicalTag NON. ThesaurusID ... Chlorphentermine Preferred Concept UI. M0004194. Registry Number. NHW07912O7. Related Numbers. 151-06-4. 461-78-9. RL11HOJ7DM. ... Chlorphentermine Hydrochloride Desopimon Pre-Sate Pharm Action. Sympathomimetics. Registry Number. NHW07912O7. Related Numbers ...
US Patent for Piperidinyl alkyne orexin receptor antagonists Patent (Patent # 8,940,898 issued January 27, 2015) - Justia...
6,730,690 and US 2004-0133011; (58) a minorex; (59) amphechloral; (60) amphetamine; (61) benzphetamine; (62) chlorphentermine ... including chlorphentermine, cloforex, clortermine, dexfenfluramine, fenfluramine, picilorex and sibutramine; and ... chlorphentermine, clobenzorex, cloforex, clominorex, clortermine, cyclexedrine, dexfenfluramine, dextroamphetamine, ...
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Cytisinicline - Wikipedia
Cytisinicline has been available in post-Soviet states for more than 40 years as an aid to smoking cessation under the brand name Tabex from the Bulgarian pharmaceutical company Sopharma AD.[3] It was first marketed in Bulgaria in 1964 and then became widely available in the then-Soviet Union.[4] In Poland, it is sold under the brand name Desmoxan, and it is also available in Canada under the brand name Cravv.[5][6] Its molecular structure has some similarity to that of nicotine, and it has similar pharmacological effects. Like the smoking cessation aid varenicline, cytisinicline is a partial agonist of nicotinic acetylcholine receptors (nAChRs).[7] Cytisinicline has a short half-life of 4.8 hours,[8] As a result, the extract provides smokers with satisfaction similar to smoking a cigarette, alleviating the urge to smoke and reducing the severity of nicotine withdrawal symptoms, while also reducing the reward experience of any cigarettes smoked.[9] Cytisinicline is rapidly eliminated from the ...
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Alveolar macrophages3
- Biochemical characteristics of rat alveolar macrophages with chlorphentermine-induced phospholipidosis: variations with increasing cell size. (cdc.gov)
- Experiments were described using centrifugal elutriation to study chlorphentermine (461789) induced phospholipidosis in alveolar macrophages from male Long-Evans-hooded-rats treated 5 days a week for 4 weeks with chlorphentermine, 30mg/kg intraperitoneally. (cdc.gov)
- Multinucleation in alveolar macrophages from rats treated with chlorphentermine. (cdc.gov)