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British Journal of Pharmacology Apr 1972Studies with methaqualone and dimethylquinazolone showed them to possess both central and peripheral muscle relaxant activity, the latter only at high dose levels. They...
Studies with methaqualone and dimethylquinazolone showed them to possess both central and peripheral muscle relaxant activity, the latter only at high dose levels. They selectively inhibited polysynaptic reflexes and were more potent than mephenesin.
Topics: Animals; Cats; Depression, Chemical; Ketones; Mephenesin; Methaqualone; Mice; Muscle Relaxants, Central; Neuromuscular Depolarizing Agents; Quinazolines; Rabbits; Reflex
PubMed: 5041454
DOI: 10.1111/j.1476-5381.1972.tb07318.x -
The Journal of Biological Chemistry Feb 2002Although microsomal triglyceride transfer protein (MTP) and newly synthesized triglyceride (TG) are critical for co-translational targeting of apolipoprotein B (apoB100)...
The late addition of core lipids to nascent apolipoprotein B100, resulting in the assembly and secretion of triglyceride-rich lipoproteins, is independent of both microsomal triglyceride transfer protein activity and new triglyceride synthesis.
Although microsomal triglyceride transfer protein (MTP) and newly synthesized triglyceride (TG) are critical for co-translational targeting of apolipoprotein B (apoB100) to lipoprotein assembly in hepatoma cell lines, their roles in the later stages of lipoprotein assembly remain unclear. Using N-acetyl-Leu-Leu-norleucinal to prevent proteasomal degradation, HepG2 cells were radiolabeled and chased for 0-90 min (chase I). The medium was changed and cells chased for another 150 min (chase II) in the absence (control) or presence of Pfizer MTP inhibitor CP-10447 (CP). As chase I was extended, inhibition of apoB100 secretion by CP during chase II decreased from 75.9% to only 15% of control (no CP during chase II). Additional studies were conducted in which chase I was either 0 or 90 min, and chase II was in the presence of [(3)H]glycerol and either BSA (control), CP (inhibits both MTP activity and TG synthesis),BMS-1976360-1) (BMS) (inhibits only MTP activity), or triacsin C (TC) (inhibits only TG synthesis). When chase I was 0 min, CP, BMS, and TC reduced apoB100 secretion during chase II by 75.3, 73.9, and 53.9%. However, when chase I was 90 min, those agents reduced apoB100 secretion during chase II by only 16.0, 19.2, and 13.9%. Of note, all three inhibited secretion of newly synthesized TG during chase II by 80, 80, and 40%, whether chase I was 0 or 90 min. In both HepG2 cells and McA-RH7777 cells, if chase I was at least 60 min, inhibition of TG synthesis and/or MTP activity did not affect the density of secreted apoB100-lipoproteins under basal conditions. Oleic acid increased secretion of TG-enriched apoB100-lipoproteins similarly in the absence or presence of either of CP, BMS, or TC. We conclude that neither MTP nor newly synthesized TG is necessary for the later stages of apoB100-lipoprotein assembly and secretion in either HepG2 or McA-RH7777 cells.
Topics: Apolipoprotein B-100; Apolipoproteins B; Carrier Proteins; Cell Line; Humans; Lipid Metabolism; Methaqualone; Protein Biosynthesis; Triazenes; Triglycerides
PubMed: 11704664
DOI: 10.1074/jbc.M107460200 -
British Medical Journal Mar 1969
Clinical Trial
Topics: Barbiturates; Diphenhydramine; Electroencephalography; Humans; Methaqualone; Sleep; Sleep, REM
PubMed: 4306021
DOI: 10.1136/bmj.1.5646.781 -
Period, age, and cohort effects on substance use among young Americans: a decade of change, 1976-86.American Journal of Public Health Oct 1988In an earlier article in this Journal, we reported analyses that differentiated among period, age, and cohort effects on substance use among American youth 18 to 24...
In an earlier article in this Journal, we reported analyses that differentiated among period, age, and cohort effects on substance use among American youth 18 to 24 years old, from the high school classes of 1976 to 1982 during the period of 1976 to 1982. The present analyses extend the classes and years to 1986, and the age range to 18-28. A cohort-sequential design is employed, based on annual surveys of nationally representative samples of high school seniors, plus annual follow-up surveys of each senior class. Twelve different classes of drugs, both licit and illicit, are examined. Several different types of period, age, and cohort effects over the last decade are identified. Alcohol use (monthly and occasions of heavy use), and the use of marijuana, cocaine, amphetamines, methaqualone, barbiturates, LSD, psychedelics other than LSD, and tranquilizers all showed period effects. Occasions of heavy drinking, cigarette smoking, monthly and daily use of alcohol, and annual prevalence of cocaine, amphetamines, barbiturates, LSD, and narcotics other than heroin showed age effects. Class effects were seen for cigarette smoking and daily marijuana use.
Topics: Adolescent; Adult; Age Factors; Alcohol Drinking; Amphetamine; Cocaine; Humans; Hypnotics and Sedatives; Illicit Drugs; Lysergic Acid Diethylamide; Marijuana Smoking; Narcotics; Smoking; Tranquilizing Agents; United States
PubMed: 3421387
DOI: 10.2105/ajph.78.10.1315 -
Japanese Journal of Pharmacology Apr 1988We investigated the characteristics of physical dependence on methaqualone. Rats were made physically dependent on methaqualone by the use of the drug-admixed food (DAF)...
We investigated the characteristics of physical dependence on methaqualone. Rats were made physically dependent on methaqualone by the use of the drug-admixed food (DAF) method for 33 days. Pentobarbital, barbital, ethanol and diazepam were cross-administered against methaqualone to evaluate the degree of suppression of methaqualone withdrawal signs as an index for the cross-physical dependence liability of these drugs to methaqualone. To evaluate the cross-physical dependence liability, we used AUC of body weight loss and withdrawal scores between the first cross-administration (9 hr after the withdrawal) and 27 hr after the withdrawal. AUC of weight loss was significantly suppressed by the four test drugs as compared to each control. Withdrawal scores were also significantly inhibited by the cross-administration of barbital, ethanol and diazepam. Considering that the rats given barbital or ethanol fell asleep after the cross-administration, diazepam seems to cause the strongest suppression of methaqualone withdrawal signs among the four test drugs. Thus, physical dependence on methaqualone may be similar by nature to that on benzodiazepines rather than barbiturates and alcohol.
Topics: Animals; Barbital; Diazepam; Ethanol; Male; Methaqualone; Pentobarbital; Postural Balance; Psychomotor Performance; Rats; Rats, Inbred Strains; Substance Withdrawal Syndrome; Substance-Related Disorders
PubMed: 3404770
DOI: 10.1254/jjp.46.403 -
British Medical Journal Apr 1967
Topics: Diphenhydramine; Humans; Male; Methaqualone; Middle Aged; Tranquilizing Agents
PubMed: 6020844
DOI: 10.1136/bmj.2.5544.112-b -
British Medical Journal Aug 1973
Topics: Cerebrospinal Fluid Proteins; Electromyography; Humans; Methaqualone; Muscular Atrophy; Peripheral Nervous System Diseases
PubMed: 4353243
DOI: No ID Found -
International Health Mar 2016This study was designed to identify the extent to which self-reported Mandrax use impacts condom-use beliefs amongst South African prison inmates.
BACKGROUND
This study was designed to identify the extent to which self-reported Mandrax use impacts condom-use beliefs amongst South African prison inmates.
METHODS
Participants were inmates from four prisons in the provinces of KwaZulu-Natal and Mpumalanga. In total, 357 inmates participated in the parent study of which 121 are included in this analysis based on their self-reported use of Mandrax. The questionnaire was developed in English, translated into Zulu, and back translated into English. Age significantly predicted the use of Mandrax: younger prison inmates reported higher use. Linear regression analysis was conducted to determine whether the use of Mandrax was associated with length of incarceration and other demographic variables, as well as participants' self-reported condom use beliefs behavior.
RESULTS
Regression results indicated that two factors operationalizing condom-use beliefs were impacted by Mandrax use: 1) it is important to use condoms every time you have sex (p<0.01); 2) condoms work well to prevent the spread of HIV (p<0.02). Both factors were also inversely related to Mandrax use.
CONCLUSION
STI prevention programs among prison inmates that seek to promote safer sex behaviors among men must address attitudes to condom use, specifically consistent and correct use of latex condoms and reducing substance misuse.
Topics: Adolescent; Adult; Condoms; Diphenhydramine; Drug Combinations; Health Knowledge, Attitudes, Practice; Humans; Male; Methaqualone; Prisoners; Prisons; Sexually Transmitted Diseases; Socioeconomic Factors; South Africa; Substance-Related Disorders; Surveys and Questionnaires; Young Adult
PubMed: 26316220
DOI: 10.1093/inthealth/ihv048 -
Postgraduate Medical Journal Mar 1968A state-registered nurse acted as a whole-time investigator following patients through the pre-operative night in hospital and questioning them in the morning, to assess... (Clinical Trial)
Clinical Trial Comparative Study
A state-registered nurse acted as a whole-time investigator following patients through the pre-operative night in hospital and questioning them in the morning, to assess the relative merits of different medications. Two new sedatives were compared with a standard barbiturate and a placebo, and information was collected from patients who elected to have no medication to help them sleep. Subjective assessment enabled the placebo to be distinguished from the active medications, although there was little difference between these. The importance of psychological factors is discussed in relation to those patients who had no medication.
Topics: Barbiturates; Chloral Hydrate; Clinical Trials as Topic; Humans; Hypnotics and Sedatives; Methaqualone; Placebos; Preanesthetic Medication
PubMed: 4869880
DOI: 10.1136/pgmj.44.509.229 -
Canadian Medical Association Journal Mar 1970A within-subject comparison of the effects on the overnight sleep EEG of 1 tablet of Mandrax (containing methaqualone base 250 mg. and diphenhydramine hydrochloride 25...
A within-subject comparison of the effects on the overnight sleep EEG of 1 tablet of Mandrax (containing methaqualone base 250 mg. and diphenhydramine hydrochloride 25 mg.) and 200 mg. Tuinal (equal parts of quinalbarbitone sodium and amylobarbitone sodium) in 14 normal subjects is reported.Mandrax-induced sleep was not significantly different from natural sleep in the duration of light, moderate, deep and REM phases. Tuinal produced a significant reduction in REM sleep (P < 0.01) compared with natural sleep and with Mandrax-induced sleep.
Topics: Adolescent; Adult; Amobarbital; Barbiturates; Diphenhydramine; Electroencephalography; Electronic Data Processing; Female; Humans; Male; Methaqualone; Sleep, REM; Tape Recording; Time Factors
PubMed: 4314659
DOI: No ID Found