Alpha-adrenoceptors in equine digital veins: evidence for the presence of both alpha1 and alpha2-receptors mediating vasoconstriction.
Abstract: Rings of equine digital vein examined under conditions of isometric tension recording constricted to alpha-adrenoceptor agonists with an order of potency of 5-bromo-6-[2-imidazolin-2-yl-amino]-quinoxaline bitartrate (UK 14304) = noradrenaline > 6-Allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo-(4,5-d) azepine (BHT-920) > phenylephrine > dopamine > methoxamine. The maximum force generated was greatest for the non-selective agonist noradrenaline and lowest for the alpha2-selective agonist BHT-920 with the other agonists between these two extremes. Selective inactivation of alpha1-adrenoceptors (achieved by treating yohimbine-protected tissues with phenoxybenzamine) reduced the maximum responses of all agonists, the EC50 values of UK 14304, BHT-920 and noradrenaline and increased the EC50 values of phenylephrine and methoxamine. Prazosin (30 nM) had no inhibitory effect on responses to low concentrations of BHT-920 and UK 14304 and caused competitive inhibition of responses to phenylephrine and noradrenaline giving pKb values of 8.49 +/- 0.18 and 8.23 +/- 0.14, respectively. Yohimbine (0.1 microM) caused significant competitive inhibition of responses to BHT-920 and noradrenaline with calculated pKb values of 8.43 +/- 0.11 for BHT-920 and 7.43 +/- 0.31 for noradrenaline and non-competitive inhibition of responses to UK 14304. 2-[2-methoxy-1,4-benzodioxan-2-yl]-2-imidazoline (RX 821002; 10 nM) caused competitive inhibition of responses to BHT-920 (pKb 9.04 +/- 0.27) and dopamine (pKb 8.2 +/- 0.2). These data indicate that equine digital veins possess both post-synaptic alpha1 and alpha2-adrenoceptors.
Publication Date: 1997-08-01 PubMed ID: 9280371DOI: 10.1046/j.1365-2885.1997.00078.xGoogle Scholar: Lookup
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- Comparative Study
- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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The research investigates the presence of both alpha1 and alpha2-adrenoceptors in equine digital veins, which are involved in regulating the constriction of blood vessels. Their research involved different types of adrenoceptor agonists and observed their potency and effect on vein constriction.
Methodology of the Study
- The researchers examined rings of equine digital veins under conditions of isometric tension recording,
- These tissues were exposed to various alpha-adrenoceptor agonists. These agonists included substances like noradrenaline, dopamine, phenylephrine, methoxamine, and artificial chemical compounds like UK 14304 and BHT-920,
- The reactions induced in the tissues by these agonists were then measured and analyzed.
Experimental Results
- The maximum force generated was highest for the non-selective agonist noradrenaline and lowest for the alpha2-selective agonist BHT-920. Other agonists generated varied responses between these two limits,
- Selective inactivation of alpha1-adrenoceptors was achieved by treating yohimbine-protected tissues with phenoxybenzamine, which reduced the maximum responses of the receptors to all agonists,
- The EC50 values – the concentration of drug that gives half-maximum response – of UK 14304, BHT-920, and noradrenaline decreased whilst those of phenylephrine and methoxamine increased upon selective inactivation of alpha1-adrenoceptors,
- Prazosin was observed to have no inhibitory effect on responses to low concentrations of BHT-920 and UK 14304 but caused competitive inhibition of responses to phenylephrine and noradrenaline,
- Yohimbine showed significant competitive inhibition of responses to BHT-920 and noradrenaline, and non-competitive inhibition of responses to UK 14304.
Study Conclusion
- From the results of this research, it can be concluded that equine digital veins possess both post-synaptic alpha1 and alpha2-adrenoceptors,
- These findings provide an understanding of the vasoconstrictive activities of these adrenoceptors in equine digital veins. This can be useful to understand in diseases and conditions related to blood flow constriction or dilation in horses.
Cite This Article
APA
Elliott J.
(1997).
Alpha-adrenoceptors in equine digital veins: evidence for the presence of both alpha1 and alpha2-receptors mediating vasoconstriction.
J Vet Pharmacol Ther, 20(4), 308-317.
https://doi.org/10.1046/j.1365-2885.1997.00078.x Publication
Researcher Affiliations
- Department of Veterinary Basic Sciences, Royal Veterinary College, London, UK.
MeSH Terms
- Adrenergic alpha-Agonists / pharmacology
- Adrenergic alpha-Antagonists / pharmacology
- Animals
- Azepines / pharmacology
- Binding, Competitive
- Brimonidine Tartrate
- Dopamine / pharmacology
- Horses / metabolism
- Idazoxan / analogs & derivatives
- Idazoxan / pharmacology
- In Vitro Techniques
- Isometric Contraction / drug effects
- Methoxamine / pharmacology
- Muscle, Smooth, Vascular / drug effects
- Norepinephrine / pharmacology
- Phenylephrine / pharmacology
- Prazosin / pharmacology
- Quinoxalines / pharmacology
- Receptors, Adrenergic, alpha-1 / drug effects
- Receptors, Adrenergic, alpha-1 / metabolism
- Receptors, Adrenergic, alpha-2 / drug effects
- Receptors, Adrenergic, alpha-2 / metabolism
- Vasoconstriction / drug effects
- Veins / drug effects
- Veins / metabolism
- Yohimbine / pharmacology
Citations
This article has been cited 4 times.- Klotz JL, Aiken GE, Bussard JR, Foote AP, Harmon DL, Goff BM, Schrick FN, Strickland JR. Vasoactivity and Vasoconstriction Changes in Cattle Related to Time off Toxic Endophyte-Infected Tall Fescue. Toxins (Basel) 2016 Sep 22;8(10).
- Menzies-Gow NJ, Wray H, Bailey SR, Harris PA, Elliott J. The effect of tumour necrosis factor-α and insulin on equine digital blood vessel function in vitro. Inflamm Res 2014 Aug;63(8):637-47.
- Marková S, Lanier HC, Escalante MA, da Cruz MOR, Horníková M, Konczal M, Weider LJ, Searle JB, Kotlík P. Local adaptation and future climate vulnerability in a wild rodent. Nat Commun 2023 Nov 29;14(1):7840.
- Wolff CB, Collier DJ, Shah M, Saxena M, Brier TJ, Kapil V, Green D, Lobo M. A Discussion on the Regulation of Blood Flow and Pressure. Adv Exp Med Biol 2016;876:129-135.
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