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9. The conversion of 2-chloroalkylamine analogues of oxotremorine to aziridinium ions and their interactions with muscarinic receptors in the guinea pig ileum.

Author

Ringdahl, B, Resul, B, Ehlert, F J, Jenden, D J, and Dahlbom, R

Abstract

Two mustard analogues of oxotremorine, N-[4-(2-chloroethylmethylamino)-2-butynyl]-2-pyrrolidone (BM 123) and N-[4-(2-chloromethylpyrrolidino)-2-butynyl]-2-pyrrolidone (BM 130), were synthesized. BM 123 and BM 130 cyclize in neutral aqueous solution to aziridinium ions. These aziridinium ions are potent stimulants of the guinea pig ileum. This agonist activity is unaffected by hexamethonium but is inhibited by methylatropine and by pretreatment of solutions of BM 123 and BM 130 with thiosulfate. The parent 2-chloroalkylamines and the alcohols formed by hydrolysis of the aziridinium ions have very weak pharmacological effects. Incubation of the isolated guinea pig ileum for 30 min with BM 123 at 20 microM and 2 microM caused 94% and 48% receptor alkylation, respectively, as calculated from the shift in the agonist dose-response curve. Similar incubations with BM 130 at 20 microM and 5 microM alkylated 85% and 63% of the receptors. No recovery from this apparent blockade was observed over a 4-hr time period. These calculated receptor occupancies by BM 123 and BM 130 agreed with those estimated from reduction of [3H] (-)-3-quinuclidinyl benzilate binding to homogenates of the ileum following exposure to BM 123 and BM 130. Methylatropine (20 nM) protected against the irreversible actions of BM 123 and BM 130. In homogenates of the guinea pig ileum, BM 123 and BM 130 also caused a selective reduction in the binding capacity of [3H]N-methylscopolamine without significantly affecting the apparent affinity. This inhibitory effect persisted after extensive washing. BM 130 was a weak agonist at nicotinic receptors of the frog rectus abdominis muscle, whereas BM 123 was almost inactive. In conclusion, BM 123 and BM 130 are potent and specific muscarinic agonists that bind irreversibly to muscarinic receptors.

Published
1984

10. Synthesis and pharmacology of 1-(2-thioxopyrrolidino)-4-pyrrolidino-2-butyne, the thiolactam analogue of oxotremorine

Author

LINDEKE, B, KARLÉN, B, DAHLBOM, R, GREEN, R, and JENDEN, D J

Abstract

The thiolactam analogue of oxotremorine (I) has been prepared and examined for muscarinic activity in mice and on guinea-pig ileal preparations. It is inactive in itself, but is transformed in vivoto oxotremorine (II), which has been identified in the urine of mice. The urine also contains 1-(2-oxopyrrolidino)-4-pyrrolidino-2-butanone (III) which is formed non-enzymatically from I under acidic conditions, but does not display any acetylcholine-like properties in vivoor in vitro.Oxotremorine is not formed from I in vitro.

Published
1972
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11. Potential antiparkinsonism agents. Quinuclidinyl benzhydryl ethers

Author

Dahlbom R, Nilsson Jl, and Wågermark J

Subjects
Atropine, Quinuclidines, Chemistry, Guinea Pigs, Parasympatholytics, Pupil, In Vitro Techniques, Acetylcholine, Mice, Diphenhydramine, Ileum, Drug Discovery, Histamine H1 Antagonists, Molecular Medicine, Organic chemistry, Animals, Tremorine, Ethers
Published
1969

33. Synthetic inhibitors of alcohol dehydrogenase. Pyrazoles containing an unsaturated hydrocarbon residue in the 4-position.

Author

Tolf BR, Dahlbom R, Theorell H, and Akeson A

Subjects
Alcohol Dehydrogenase, Animals, Chemical Phenomena, Chemistry, Horses, In Vitro Techniques, Kinetics, Liver enzymology, Pyrazoles pharmacology, Alcohol Oxidoreductases antagonists & inhibitors, Pyrazoles chemical synthesis
Abstract

A series of pyrazoles containing an unsaturated hydrocarbon residue in the 4-position has been synthesized and tested for ability to inhibit the activity of the enzyme liver alcohol dehydrogenase. These compounds were found to be less active than the corresponding saturated analogues.

Published
1982
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38. Acetylene compounds of potential pharmacological value. XL. N-(tert-aminoalkynyl)-substituted 3-isothiazolidinone-1,1-dioxides and tetrahydro-1,2-thiazin-3-one-1,1-dioxides.

Author

Lindeke B, Dahlbom R, and Ringdahl B

Subjects
Animals, Chemical Phenomena, Chemistry, Chromans pharmacology, Cyclic S-Oxides pharmacology, Guinea Pigs, Ileum drug effects, In Vitro Techniques, Male, Mice, Muscle Contraction drug effects, Structure-Activity Relationship, Thiazines pharmacology, Thiazoles pharmacology, Anticonvulsants, Benzopyrans chemical synthesis, Carbachol antagonists & inhibitors, Chromans chemical synthesis, Cyclic S-Oxides chemical synthesis, Muscle, Smooth drug effects, Thiazines chemical synthesis, Thiazoles chemical synthesis
Published
1987

39. Acetylene compounds of potential pharmacological value. XXIX. Stereoselectivity of N-(1-alkyl-4-pyrrolidino-2-butynyl)-substituted 2-pyrrolidones and succinimides as oxotremorine antagonists.

Author

Ringdahl B and Dahlbom R

Subjects
Animals, Chemical Phenomena, Chemistry, Drug Evaluation, Preclinical, Mice, Mydriatics pharmacology, Pyrrolidinones pharmacology, Stereoisomerism, Succinimides pharmacology, Acetylene, Mydriatics chemical synthesis, Oxotremorine antagonists & inhibitors, Pyrrolidinones chemical synthesis, Succinimides chemical synthesis
Published
1979

41. Muscarinic activity in the isolated guinea pig ileum of some carboxamides related to oxotremorine.

Author

Ringdahl B, Resul B, Jenden DJ, and Dahlbom R

Subjects
Animals, Dibenzylchlorethamine pharmacology, Guinea Pigs, Ileum drug effects, In Vitro Techniques, Male, Muscle Contraction drug effects, Oxotremorine pharmacology, Parasympatholytics pharmacology, Muscle, Smooth drug effects, Oxotremorine analogs & derivatives, Parasympathomimetics, Receptors, Cholinergic drug effects, Receptors, Muscarinic drug effects
Abstract

A series of structural analogues of the potent oxotremorine-like agent N-(4-pyrrolidino-2-butynyl)-N-methyl-acetamide (1) was investigated for muscarinic activity in the isolated guinea pig ileum. Substitution of larger alkyl groups for the acetyl methyl group of 1 results in an attenuation of muscarinic potency. The observation that the agonist N-(4-dimethylamino-2-butynyl)-N-methylpropionamide (6) has a dissociation constant (KA = 5.1 X 10(-5) M), estimated after elimination of spare receptors with dibenamine, similar to that of the antagonist N-(4-dimethylamino-2-butynyl)-N-methyl-2,2-dimethylpropionamide (11) suggests that the decrease in muscarinic agonist activity with increasing substitution is due mainly to a loss of efficacy. The N-methyl group of 1 is essential for muscarinic activity since its replacement by a hydrogen atom or an ethyl group yields antagonists.

Published
1982
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42. Cyclizing compounds. V. Tertiary haloalkylamine derivatives related to the tricyclic psychopharmacological agents promazine, imipramine and amitriptyline.

Author

Holmberg B, Lindborg B, Dahlbom R, and Ross SB

Subjects
Amitriptyline analogs & derivatives, Animals, Behavior, Animal drug effects, Brain Chemistry drug effects, Chemical Phenomena, Chemistry, Imipramine analogs & derivatives, Male, Mice, Promazine analogs & derivatives, Antidepressive Agents, Tricyclic chemical synthesis
Published
1984

44. Muscarinic activity of some secondary and tertiary amines and quaternary ammonium salts structurally related to oxotremorine.

Author

Resul B, Ringdahl B, Dahlbom R, and Jenden DJ

Subjects
Animals, Guinea Pigs, Ileum drug effects, In Vitro Techniques, Male, Mice, Mice, Inbred Strains, Muscle Contraction drug effects, Structure-Activity Relationship, Tremor chemically induced, Amines pharmacology, Oxotremorine pharmacology, Receptors, Cholinergic drug effects, Receptors, Muscarinic drug effects
Abstract

A number of secondary and tertiary amines as well as quaternary ammonium compounds, obtained by structural modification of the amino group of oxotremorine (1) and its acetamide analogue (14), were investigated for muscarinic and antimuscarinic activity in vivo and in vitro. For the quaternary ammonium analogues, decrease of in vitro muscarinic potency is well correlated with increase of the size of the quaternary ammonium group, as estimated from increments in apparent molal volumes. A similar decrease of muscarinic potency with increasing substitution at the nitrogen atom is generally observed for the secondary and tertiary amines. For the latter the reduction in muscarinic activity appears to be due to loss of efficacy, since the higher homologues are partial agonists or antagonists. There is a highly significant correlation between muscarinic activity in vitro and central tremorogenic activity of the tertiary amines.

Published
1983
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45. Cyclizing compounds. IV. Tertiary N-(2-(3,4,5-trimethoxybenzoyloxy)ethyl)-N-haloalkylamines with hemicholinium-like activity.

Author

Lindborg B, Johansson JG, and Dahlbom R

Subjects
Acetylcholine metabolism, Animals, Brain metabolism, Brain Chemistry drug effects, Cats, Chemical Phenomena, Chemistry, Choline metabolism, Cyclization, Depression, Chemical, In Vitro Techniques, Methods, Mice, Synaptosomes metabolism, Tritium, Amines chemical synthesis, Amines pharmacology, Amines toxicity
Published
1974

47. The pharmacological assessment of a new, potent oxotremorine analogue in mice and rats.

Author

Resul B, Lewander T, Ringdahl B, Zetterström T, and Dahlbom R

Subjects
Animals, Body Temperature drug effects, Dose-Response Relationship, Drug, Guinea Pigs, Ileum drug effects, In Vitro Techniques, Male, Mice, Mice, Inbred Strains, Muscle Contraction drug effects, Oxotremorine metabolism, Rats, Rats, Inbred Strains, Oxotremorine analogs & derivatives, Oxotremorine pharmacology, Parasympathomimetics pharmacology
Abstract

Some of the central and peripheral effects of oxotremorine (OT) and its azetidine analogue, N-[4-azetidinyl)-2-butynyl]-2-pyrrolidone (BM 120), were compared in mice and rats. BM 120 was found to be about twice as potent as OT and to have a somewhat longer duration of action. All its effects were antagonized by pretreatment with atropine sulphate. BM 120 acted as powerful muscarinic agonist on the isolated guinea pig ileum.

Published
1982
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49. Acetylene compounds of potential pharmacological value. XXVII. Stereoselectivity of oxotremorine antagonists containing a chiral pyrrolidine group.

Author

Ringdahl B and Dahlbom R

Subjects
Animals, Chemical Phenomena, Chemistry, Drug Evaluation, Preclinical, Mice, Oxotremorine analogs & derivatives, Pyrrolidines pharmacology, Rats, Stereoisomerism, Succinimides pharmacology, Motor Activity drug effects, Mydriatics chemical synthesis, Oxotremorine antagonists & inhibitors, Pyrrolidines chemical synthesis
Published
1978

50. Acetylene compounds of potential pharmacological value. XXX. Synthesis and pharmacological properties of N-(4-pyrrolidino-2-pentynyl)-substituted 2-pyrrolidone and succinimide.

Author

Resul B, Ringdahl B, and Dahlbom R

Subjects
Animals, Chemical Phenomena, Chemistry, Mice, Oxotremorine antagonists & inhibitors, Pyrrolidinones chemical synthesis, Succinimides chemical synthesis, Tremor chemically induced, Tremor drug therapy, Acetylene analogs & derivatives, Pyrrolidinones pharmacology, Succinimides pharmacology
Published
1979

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