doi: 10.1007/BF01968110.
Inhibition of histamine methylation in vivo by the dimaprit analog, SKF Compound 91488
- PMID: 161853
- DOI: 10.1007/BF01968110
Item in Clipboard
Inhibition of histamine methylation in vivo by the dimaprit analog, SKF Compound 91488
Agents Actions.
1979 Dec.
Abstract
The Dimaprit analog, S-[4-(N,N-dimethylamino)-butyl]isothiurea (SKF Compound 91488), which is a noncompetitive inhibitor (Ki, 0.9 microM) of histamine-N-methyltransferase in vitro, inhibited the methylation of labeled histamine in mice. When administered in combination with the diamine oxidase inhibitor, aminoguanidine, an almost complete block of histamine metabolism was observed. The inhibition was dependent on dose of drug and was apparent with doses of 50 mg/kg and greater. Since Compound 91488 is reported to have no agonist activity of its own, the drug may help to identify the actions of histamine released from endogenous stores in response to physiological and pathological stimuli.
Similar articles
-
Inhibition of histamine-N-methyltransferase and histaminase (diamine oxidase) by a new histamine H2-receptor agonist, Dimaprit.Biochem Pharmacol. 1977 Nov 1;26(21):2075-8. doi: 10.1016/0006-2952(77)90021-1. Biochem Pharmacol. 1977. PMID: 411497 No abstract available.
-
Evidence for a role of endogenous histamine in central cardiovascular regulation: inhibition of histamine-N-methyltransferase by SKF 91488.J Pharmacol Exp Ther. 1981 Feb;216(2):315-20. J Pharmacol Exp Ther. 1981. PMID: 6450831
-
Histamine N-methyltransferase inhibitor potentiates histamine- and antigen-induced airway microvascular leakage in guinea pigs.J Allergy Clin Immunol. 1995 Dec;96(6 Pt 1):910-6. doi: 10.1016/s0091-6749(95)70228-8. J Allergy Clin Immunol. 1995. PMID: 8543749
-
Histamine N-methyltransferase controls the contractile response of guinea pig trachea to histamine.J Pharmacol Exp Ther. 1992 Jun;261(3):1268-72. J Pharmacol Exp Ther. 1992. PMID: 1534842
-
Histamine N-Methyltransferase in the Brain.Int J Mol Sci. 2019 Feb 10;20(3):737. doi: 10.3390/ijms20030737. Int J Mol Sci. 2019. PMID: 30744146 Free PMC article. Review.
Cited by
-
Histamine H3 receptor agonists decrease hypothalamic histamine levels and increase stereotypical biting in mice challenged with methamphetamine.Neurochem Res. 2011 Oct;36(10):1824-33. doi: 10.1007/s11064-011-0500-8. Epub 2011 May 15. Neurochem Res. 2011. PMID: 21573995 Free PMC article.
-
Two polymorphic forms of human histamine methyltransferase: structural, thermal, and kinetic comparisons.Structure. 2001 Sep;9(9):837-49. doi: 10.1016/s0969-2126(01)00643-8. Structure. 2001. PMID: 11566133 Free PMC article.
-
Histamine N-methyltransferase Modulates Human Bronchial Smooth Muscle Contraction.Mediators Inflamm. 1994;3(2):125-9. doi: 10.1155/S0962935194000153. Mediators Inflamm. 1994. PMID: 18472930 Free PMC article.
-
Histamine N-methyltransferase (HNMT) as a potential auxiliary biomarker for predicting adaptability to anti-HER2 drug treatment in breast cancer patients.Biomark Res. 2025 Jan 9;13(1):7. doi: 10.1186/s40364-024-00715-5. Biomark Res. 2025. PMID: 39789599 Free PMC article.
-
Central cardiovascular responses of histamine and homodimaprit in normal and hypophysectomized rats.Agents Actions. 1990 Nov;31(3-4):243-8. doi: 10.1007/BF01997615. Agents Actions. 1990. PMID: 1982202