The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Dso-16     1-[4-(2-chloroethyl-methyl- amino)but-2...

Synonyms: Dso 16, AG-J-19219, KST-1B3924, AC1Q3BII, CTK4H3466, ...
This record was replaced with 169658.
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of 1-[4-(2-chloroethyl-methyl-amino)but-2-ynyl]pyrrolidin-2-one


High impact information on 1-[4-(2-chloroethyl-methyl-amino)but-2-ynyl]pyrrolidin-2-one

  • The kinetics of the alkylation of muscarinic receptors by BM 123 were consistent with a model in which the aziridinium ion rapidly forms reversible complexes with superhigh high and low affinity sites which slowly convert to covalent complexes [2].
  • 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 [3].
  • BM 130 was a weak agonist at nicotinic receptors of the frog rectus abdominis muscle, whereas BM 123 was almost inactive [3].
  • The role of muscarinic receptors in the regulation of (3H)-acetylcholine (3H-Ach) release from the hippocampus was investigated with the irreversible cholinergic agonist BM-123 (N-[4(2-chloroethylmethylamino)-2-butynyl]2-pyrrolidone) [4].
  • Muscarinic receptors from rat cerebral cortex were found to recover from alkylation by the specific ligand N-[-(2-chloroethyl-methylamino)-2-butynyl]-2-pyrrolidone (BM 123) without the benefit of cellular integrity, i.e., in washed membranes incubated at 37 degrees C for relatively long times (days) [5].

Biological context of 1-[4-(2-chloroethyl-methyl-amino)but-2-ynyl]pyrrolidin-2-one

  • It was possible to alkylate the high and low affinity sites selectively with BM 123 by taking advantage of kinetic differences in the rates of alkylation of these two sites [2].
  • Thus, central potency of 2-haloethylamines such as BR 401 and BM 123 is critically dependent not only on the rate of cyclization, but also on the route of administration [6].
  • The reversible binding characteristics of both BM 123 and BM 123A were investigated in competitive binding experiments with N-[3H]methylscopolamine at 0 degree C, conditions under which little or no receptor alkylation occurs [7].
  • Upon i.v. administration, BR 401 was 2- to 3-fold more potent than oxotremorine and 10 to 20 times more potent than BM 123 in producing central (tremor and analgesia) and peripheral (salivation) muscarinic effects [6].
  • Kinetic studies of the interaction of BM 123 with homogenates of the rat cerebral cortex in vitro showed that the half-time for the loss of [3H]1-QNB binding sites increased from 10 to 45 min as the concentration of BM 123 decreased from 10 to 1 microM [8].

Anatomical context of 1-[4-(2-chloroethyl-methyl-amino)but-2-ynyl]pyrrolidin-2-one


Analytical, diagnostic and therapeutic context of 1-[4-(2-chloroethyl-methyl-amino)but-2-ynyl]pyrrolidin-2-one


  1. Spontaneous regeneration of free muscarinic receptor after alkylation by BM 123. I. Recovery in vivo and in cell culture. Waite, J.J., Jenden, D.J. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  2. The binding of a 2-chloroethylamine derivative of oxotremorine (BM 123) to muscarinic receptors in the rat cerebral cortex. Ehlert, F.J., Jenden, D.J. Mol. Pharmacol. (1985) [Pubmed]
  3. The conversion of 2-chloroalkylamine analogues of oxotremorine to aziridinium ions and their interactions with muscarinic receptors in the guinea pig ileum. Ringdahl, B., Resul, B., Ehlert, F.J., Jenden, D.J., Dahlbom, R. Mol. Pharmacol. (1984) [Pubmed]
  4. Effect of irreversible loss of muscarinic receptors on (3H)-acetylcholine release from the hippocampus. Sethy, V.H., Hyslop, D.K. Neuropharmacology (1990) [Pubmed]
  5. Spontaneous regeneration of free muscarinic receptor after alkylation by BM 123. II. Recovery in broken cell preparations. Waite, J.J., Jenden, D.J. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  6. Muscarinic actions of an N-methyl-N-2-bromoethylamino analog of oxotremorine (BR 401) in the mouse. Ringdahl, B., Jenden, D.J. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  7. Effects of an alkylating derivative of oxotremorine (BM 123A) on heart rate, muscarinic receptors and adenylate cyclase activity in the rabbit myocardium. Ehlert, F.J. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  8. An alkylating derivative of oxotremorine interacts irreversibly with the muscarinic receptor. Ehlert, F.J., Jenden, D.J., Ringdahl, B. Life Sci. (1984) [Pubmed]
WikiGenes - Universities