Skip to main content
Log in

Inhibition of noradrenaline release from the sympathetic nerves of the human saphenous vein by presynaptic histamine H3 receptors

Naunyn-Schmiedeberg's Archives of Pharmacology Aims and scope Submit manuscript

Summary

The human saphenous vein was used to examine whether presynaptic histamine receptors can modulate noradrenaline release and, if so, to determine their pharmacological characteristics. Strips of this blood vessel were incubated with [3H]noradrenaline and subsequently superfused with physiological salt solution containing desipramine and corticosterone. Electrically (2 Hz) evoked 3H overflow was inhibited by histamine and the H3 receptor agonist R-(−)-α-methylhistamine. Histamine-induced inhibition of electrically evoked tritium overflow was not affected by α2-adrenoceptor blockade by rauwolscine. S-(+)-α-methylhistamine (up to 10 μmol/l) as well as the histamine H1 and H2 receptor agonists 2-(2-thiazolyl)ethylamine (up to 3 μmol/l) and dimaprit (up to 30 μmol/l), respectively, were ineffective. The selective histamine H3 receptor antagonist thioperamide abolished the inhibitory effect of histamine. The histamine H2 and H1 receptor antagonists ranitidine and pheniramine, respectively, did not affect the histamine-induced inhibition of evoked tritium overflow. The present results are compatible with the suggestion that the sympathetic nerves of the human saphenous vein are endowed with inhibitory presynaptic histamine receptors of the H3 class.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  • Arrang JM, Garbarg M, Schwartz JC (1983) Auto-inhibition of brain histamine release by a novel class (H3) of histamine receptor. Nature 302:832–837

    Google Scholar 

  • Arrang JM, Garbarg M, Lancelot JC, Lecomte JM, Pollard H, Robba M, Schunack W, Schwartz JC (1987) Highly potent and selective ligands for histamine H3 receptors. Nature 327:117–123

    Google Scholar 

  • Endo T, Starke K, Bangerter A, Taube HD (1977) Presynaptic receptor systems on the noradrenergic neurones of the rabbit pulmonary artery. Naunyn-Schmiedeberg's Arch Pharmacol 296:229–247

    Google Scholar 

  • Ercan ZS, Türker RK (1981) Alteration by histamine receptor agonists of the release of adrenergic transmitter in the isolated perfused rabbit kidney. Arch Int Pharmacodyn 249:203–212

    Google Scholar 

  • Göthert M, Hentrich F (1985) Identification of presynaptic β2-adrenoceptors on the sympathetic nerve fibres of the human pulmonary artery. Br J Pharmac 85:933–941

    Google Scholar 

  • Göthert M, Schlicker E, Hentrich F, Rohm N, Zerkowski HR (1984) Modulation of noradrenaline release in human saphenous vein via presynaptic α2-adrenoceptors. Eur J Pharmacol 102:261–267

    Google Scholar 

  • Haaksma EEJ, Leurs R, Timmerman H (1990) Histamine receptors, subclasses and specific ligands. Pharmac Ther 47:73–104

    Google Scholar 

  • Hill SJ (1990) Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol Rev 42:45–83

    Google Scholar 

  • Holcslaw TL, Lassiter D (1987) Evidence for presynaptic inhibitory histamine (H2) receptors in the rat hindquarter vasculature. J Cardiovasc Pharmacol 9:651–660

    Google Scholar 

  • Ishikawa S, Sperelakis N (1987) A novel class (H3) of histamine receptors on perivascular nerve terminals. Nature 327:158–160

    Google Scholar 

  • Lokhandwala MF (1978) Inhibition of sympathetic nervous system by histamine: studies with H1- and H2-receptor antagonists. J Pharmacol Exp Ther 206:115–122

    Google Scholar 

  • McGrath MA, Shepherd JT (1976) Inhibition of adrenergic neurotransmission in canine vascular smooth muscle by histamine. Circulation Res 39:566–573

    Google Scholar 

  • Molderings GJ, Göthert M (1990) Mutual interaction between presynaptic α2-adrenoceptors and 5-HT1B receptors on the sympathetic nerve terminals of the rat inferior vena cava. Naunyn-Schmiedeberg's Arch Pharmacol 341:391–397

    Google Scholar 

  • Molderings GJ, Hentrich F, Göthert M (1991a) Pharmacological characterization of the imidazoline receptor which mediates inhibition of noradrenaline release in the rabbit pulmonary artery. Naunyn-Schmiedeberg's Arch Pharmacol 344:630–638

    Google Scholar 

  • Molderings GJ, Weißenborn G, Schlicker E, Göthert M (1991b) Pharmacological characterization of the inhibitory presynaptic histamine receptors on the sympathetic nerves of the human saphenous vein. Naunyn-Schmiedeberg's Arch Pharmacol 344 [Suppl]:R73 (abstr)

    Google Scholar 

  • Nauta WT, Rekker RF (1978) Structure-activity relationships of H1-receptor antagonists. In: Rocha e Silva M (ed) Handbook of experimental pharmacology. Histamine II and antihistaminics, vol XVIII. Springer, Berlin Heidelberg New York, pp 215–249

    Google Scholar 

  • Powell JR (1979) Effects of histamine on vascular sympathetic neuroeffector transmission. J Pharmacol Exp Ther 208:360–365

    Google Scholar 

  • Rand MJ, Story DF, Wong-Dusting HK (1982) Effects of histamine on the resting and stimulation-induced release of [3H]-noradrenaline in guinea-pig isolated atria. Br J Pharmacol 75:57–64

    Google Scholar 

  • Robic NW, Barker LA (1983) Evaluation of presynaptic histamine receptors in the canine renal vascular bed. J Pharmacol Exp Ther 226:712–719

    Google Scholar 

  • Schlicker E, Fink K, Hinterthaner M, Göthert M (1989) Inhibition of noradrenaline release in the rat brain cortex via presynaptic H3 receptors. Naunyn-Schmiedeberg's Arch Pharmacol 340:633–638

    Google Scholar 

  • Schlicker E, Schunack W, Göthert M (1990) Histamine H3 receptor-mediated inhibition of noradrenaline release in pig retina discs. Naunyn-Schmiedeberg's Arch Pharmacol 342:497–501

    Google Scholar 

  • Schneider D, Schlicker E, Malinowska B, Molderings G (1991) Noradrenaline release in the rat vena cava is inhibited by γ-aminobutyric acid via GABAB receptors but not affected by histamine. Br J Pharmacol 104:478–482

    Google Scholar 

  • Schwartz JC, Arrang JM, Garbarg M, Pollard H, Ruat M (1991) Histaminergic transmission in the mammalian brain. Physiol Rev 71:1–51

    Google Scholar 

  • Starke K, Göthert M, Kilbinger H (1989) Modulation of neurotansmitter release by presynaptic autoreceptors. Physiol Rev 69:864–989

    Google Scholar 

  • Timmerman H (1990) Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? J Med Chem 33:4–11

    Google Scholar 

  • Vassilev P, Staneva-Stoytcheva D, Mutafova-Yambolieva V (1991) Do H3 receptors participate in the effects of histamine on electrically evoked contractions of rat vas deferens? Gen Pharmacol 22: 643–645

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Additional information

Send offprint requests to M. Gothert at the above address

Rights and permissions

Reprints and permissions

About this article

Cite this article

Molderings, G.J., Weißenborn, G., Schlicker, E. et al. Inhibition of noradrenaline release from the sympathetic nerves of the human saphenous vein by presynaptic histamine H3 receptors. Naunyn-Schmiedeberg's Arch Pharmacol 346, 46–50 (1992). https://doi.org/10.1007/BF00167569

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00167569

Key words

Navigation