2-chloroethyl Amine Hydrochloride Research Articles

Evaluation of CB 1348 in Hodgkin's disease and allied disorders.

It has been clearly established that methylbis (β - chloroethyl) amine hydrochloride (nitrogen mustard) is an excellent supplement to radiotherapy in the treatment of Hodgkin's disease * and is also of some value in other related lymphomas and leukemias.† However, it has the disadvantages that it must be administered intravenously, that it produces marked bone marrow depression, and that it causes such side-effects as nausea, vomiting, and malaise. A chemical derivative of nitrogen mustard without such disadvantages would be extremely useful. Triethylenemelamine (TEM), which may be administered by mouth, is very toxic, and its effect is often incalculable.‡ Another nitrogen mustard derivative, β-naphthyl-bis (2-chloroethyl) amine (R 48; CB 1048), has proved of some value in Hodgkin's disease, polycythemia rubra vera. and some leukemias.§ Russian investigators have synthesized a nitrogen mustard derivative, p -bis (2-chloroethyl ) aminophenylalanine (sarcolysine), which when tested against a variety of animal tumors has exhibited antitumor activity. 12 For the

USE OF "DIBENZYLINE" AS A VASODILATOR IN PATIENTS WITH SEVERE DIGITAL ISCHEMIA

IN THE management of patients with vascular disease one naturally seeks for a vasodilator drug which will offer substantial vasodilatation in the extremities with minimal effects elsewhere. Such a drug would be particularly useful in so-called Raynaud's syndrome, where it might often obviate the need for surgical sympathectomy, especially for the upper extremity, when the operation is frequently unsatisfactory. The vasodilator effect of Dibenzyline * (N-phenoxyisopropyl-N-benzyl- β -chloroethylamine hydrochloride) has been briefly reported by several observers.† The results in a few patients in whom we tried this drug in 1951 gave promise that Dibenzyline more nearly approached the ideal than other vasodilators with which we were acquainted. This opinion was strengthened by a further use of Dibenzyline over a two-year period for 23 patients suffering from severe digital ischemia, and we, therefore, offer this account of our experiences. We feel that the drug was given a somewhat more rigorous test than

The effect of intra-arterial nitrogen-mustard therapy on human skin.

CancerVolume 6, Issue 2 p. 288-293 ArticleFree Access The effect of intra-arterial nitrogen-mustard. (Methylbis(2-chloroethyl)amine hydrochloride). Therapy on human skin Robert D. Sullivan M.D., Robert D. Sullivan M.D. National Cancer Institute, of the National Institutes of Health, Public Health Service, Federal Security Agency, Bethesda, Maryland. Present address: Memorial Center for Cancer and Allied Diseases, New York, New YorkSearch for more papers by this authorHerbert Mescon M.D., Herbert Mescon M.D. C. Willard Robinson Section of the Department of Medicine and the Dermatopathology Laboratories, Department of Dermatology, Hospital of the University of Pennsylvania, Philadelphia, PennsylvaniaSearch for more papers by this authorRalph Jones Jr. M.D., Ralph Jones Jr. M.D. C. Willard Robinson Section of the Department of Medicine and the Dermatopathology Laboratories, Department of Dermatology, Hospital of the University of Pennsylvania, Philadelphia, Pennsylvania Markle Scholar in Medical Science.Search for more papers by this author Robert D. Sullivan M.D., Robert D. Sullivan M.D. National Cancer Institute, of the National Institutes of Health, Public Health Service, Federal Security Agency, Bethesda, Maryland. Present address: Memorial Center for Cancer and Allied Diseases, New York, New YorkSearch for more papers by this authorHerbert Mescon M.D., Herbert Mescon M.D. C. Willard Robinson Section of the Department of Medicine and the Dermatopathology Laboratories, Department of Dermatology, Hospital of the University of Pennsylvania, Philadelphia, PennsylvaniaSearch for more papers by this authorRalph Jones Jr. M.D., Ralph Jones Jr. M.D. C. Willard Robinson Section of the Department of Medicine and the Dermatopathology Laboratories, Department of Dermatology, Hospital of the University of Pennsylvania, Philadelphia, Pennsylvania Markle Scholar in Medical Science.Search for more papers by this author First published: March 1953 https://doi.org/10.1002/1097-0142(195303)6:2<288::AID-CNCR2820060211>3.0.CO;2-4Citations: 14 AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat Citing Literature Volume6, Issue2March 1953Pages 288-293 ReferencesRelatedInformation

The treatment of human cancer with intra-arterial nitrogen mustard, methylbis (2-chloroethyl) amine hydrochloride, utilizing a simplified catheter technique.

The treatment of human cancer with intra-arterial nitrogen mustard, methylbis (2-chloroethyl) amine hydrochloride, utilizing a simplified catheter technique.

Adrenergic Blocking Agents. V. Synthesis of N - Benzyl - N - (1 - phenoxyisopropyl) - β - chloroethylamine Hydrochloride Labeled with C14

Adrenergic Blocking Agents. V. Synthesis of N - Benzyl - N - (1 - phenoxyisopropyl) - β - chloroethylamine Hydrochloride Labeled with C¹⁴

Triethylene melamine in the treatment of neoplastic disease; a compound with nitrogen-mustardlike activity suitable for oral and intravenous use.

THE NITROGEN mustards were introduced into medical practice in 1946 for the palliative treatment of the lymphomas, leukemias and other types of neoplastic disease.¹The most commonly administered nitrogen mustard is methyl-<i>bis</i>(2-chloroethyl) amine hydrochloride (HN2), and, since 1946, much experience has been gained from its use throughout the world.²This nitrogen mustard has found a useful place as a temporary palliative agent in the management of certain types and stages of neoplastic disease. It must be injected intravenously, and it frequently produces severe nausea and vomiting; consequently, its administration, in most cases, has been regarded as a hospital procedure. Extravasation of the injected solution will produce a prolonged and painful local reaction, and, in patients receiving repeated courses of treatment, venous thromboses and difficulty in finding suitable veins for injection may occur. The dosage must be carefully controlled, since an excessive dose will produce serious, prolonged

Effect of N,N-Dibenzyl- -Chloroethylamine Hydrochloride (Dibenamine) on Autonomic Functions and Catatonia in Schizophrenic Subjects.

1. Certain autonomic functions (B.P., P.R., skin temperature, palmar sweat response, electrical skin resistance), the signs of catatonia, and the psychiatric status of 9 patients with schizophrenic reactions, catatonic type, were evaluated before and after saline, sodium amytal, and Dibenamine infusions.

Effects of a New Congener of Dibenamine on the Actions of Sympathomimetic Amines.

Summary and Conclusions1. Drug 194 (N-benzyl-N-β-phenylisopropyl-β chloroethylamine hydrochloride), has been shown to be a potent antagonist of certain excitatory effects of a number of sympathomimetic agents. In the cat, 194 reduced or abolished pressor responses to aliphatic and aromatic amines and to catechol. In the presence of 194, all the compounds, except neosynephrine, privine, and paredrinol, manifested depressor activity.2. The effects of nerve stimulation on the nictitating membrane of the cat were less effectively blocked by 194 than were the effects of epinephrine. 194 also could prevent or interrupt nictitating membrane contractions induced by sympathomimetic amines other than epinephrine.

The Newer Nitrogen Mustards in the Treatment of Leukemia

Since the discovery by Gilman, Goodman, Lindskog, and Dougherty (1) of the chemotherapeutic effect of the nitrogen mustards on lymphosarcoma, and their application to the treatment of Hodgkin's disease by Jacobson (2), these agents have been widely used in the treatment of leukemia and the lymphomas (3-7). Because the effect of the nitrogen mustards originally employed in the therapy of neoplastic disease, although definite, was only palliative, a search for related compounds which might exert a more beneficial and more prolonged effect was instituted. In the studies of cancer chemotherapy at the Sloan-Kettering Institute certain nitrogen mustard derivatives have been shown to be effective in prolonging the survival time of mice with transmitted leukemia (8). One of these derivatives has now been examined extensively for its therapeutic value against leukemia in man, and the results are herewith reported. This new nitrogen mustard derivative, 1:3 propane diamine N N N′ N′ tetrakis-(2-chloroethyl)dihydrochloride, more commonly known as SK 136, is of about the same order of toxicity as methyl bis(2chloroethyl)amine hydrochloride, the more widely used nitrogen mustard known as HN2, in that the leukotoxic and LD50 doses were approximately the same in mice and in larger animals. It was noted, however, in rats, that with SK 136 convulsions were produced by smaller multiples of the lethal dose than with HN2. When given clincally in a dosage of 0.1 mg. per kilogram of body weight daily for four to eight doses, SK 136 usually caused much less nausea and vomiting than did HN2, but a slight degree of dizziness was experienced by most patients. This relative lack of nausea and vomiting seemed to be particularly noticeable with cases of chronic myelogenous leukemia, whereas patients with Hodgkin's disease occasionally had as much or more nausea and vomiting than they did with HN2. The dizziness generally was not severe and disappeared in one to twenty-four hours after injection. An occasional patient complained of nervousness and bad dreams following the injections, but no true hallucinations of toxic psychoses were noted. As with HN2, leukopenia and thrombocytopenia were occasionally noted. In contrast to HN2, in which increase of the amount given in a single injection to 0.2 mg. per kilogram of body weight caused no marked increase in the nausea and vomiting, doubling the dose of SK 136 caused the appearance of nausea and vomiting and severe dizziness. A closely allied derivarive, SK 137, 1:3 propane diamine-2-chloro N N N′ N′ tetrakis (2-chloroethyl) dihydrochloride, in which a chlorine was substituted for a hydrogen in the 2-position of the propane moiety, was also tested clinically. The chemotherapeutic activity of the two drugs appeared to be approximately equal, but the appearance of occasional transient toxic psychoses of twelve to seventy-two hours' duration with SK 137 caused its use to be discontinued.

Inhibitory Effect of Dibenarnine on Vasoconstrictor Substances

Summary1. Dibenzyl - β - chloroethyl amine hydrochloride (dibenamine) inhibits the vasoconstrictor action of epinephrine, as tested in the Laewen-Trendelenburg preparation in the frog. Its adrenolytic action is very potent, for it blocks even large amounts of epinephrine (50-1000 γ). 2. When the action of large amounts of epinephrine is completely inhibited by dibenamine, both hypertensin and nicotine still exhibit a marked vasoconstrictor activity. 3. The peripheral locus of action of dibenamine seems to be at the neuroeffector cells or between the postganglionic nerve endings and the latter.