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Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse.
Abstract: Hordenine is an alkaloid occurring naturally in grains, sprouting barley, and certain grasses. It is occasionally found in post race urine samples, and therefore we investigated its pharmacological actions in the horse. Hordenine (2.0 mg/kg bodyweight [bwt]) was administered by rapid intravenous (iv) injection to 10 horses. Typically, dosed horses showed a flehmen response and defecated within 60 secs. All horses showed substantial respiratory distress. Respiratory rates increased about 250 per cent and heart rates were approximately double that of resting values. All animals broke out in a sweat shortly after iv injection, but basal body temperature was not affected. These effects were transient, and the animals appeared normal within 30 mins of dosing. Treated horses were tested in a variable interval responding apparatus 30 mins after dosing and no residual stimulation or depressant effects of hordenine were apparent. Animals dosed orally with 2.0 mg/kg bwt of hordenine showed no changes in heart rate, respiratory rate, basal body temperature or behaviour. After iv injection of hordenine, (2.0 mg/kg bwt) plasma reached a maximum value of about 1.0 micrograms/ml, and declined thereafter in a biexponential fashion. Kinetics of plasma concentration satisfied the concept of a two compartment open system, with an alpha-phase half-life of about 3 mins, and a beta-phase half-life of about 35 mins. Total urinary concentrations of hordenine (free and conjugated) peaked at about 400 micrograms/ml, and then declined exponentially to background levels by 24 h after dosing.(ABSTRACT TRUNCATED AT 250 WORDS)
Publication Date: 1990-11-01 PubMed ID: 2269269DOI: 10.1111/j.2042-3306.1990.tb04312.xGoogle Scholar: Lookup The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.
The research paper revolves around Hordenine, a natural compound in grains and grasses, its effects on horses when administered intravenously, and its detection in urine samples. The authors studied the physiological and behavioural effects of Hordenine supplied to horses and its pharmacokinetic attributes.
Study Methodology and Results
- The researchers administered Hordenine to horses using rapid intravenous injection. The dosage was 2.0 mg/kg of the horse’s weight. It was given to a sample size of ten horses.
- Behavioural responses from the horses were observed within 60 seconds of Hordenine’s administration. The horses showed a flehmen reaction, which is a unique behaviour expressed by many mammals, and began to defecate.
- Significant respiratory distress was observed in all the horses. Their respiration rates shot up by around 250%, and their heart rates became twice the usual resting rates.
- The horses quickly started sweating after the intravenous injection, even though their basal body temperature remained unaffected.
Transient Effects and Absence of Long-Term Impact
- All the effects were momentary and disappeared within 30 minutes of the dose, after which time the horses appeared normal.
- To test any lingering or hidden impacts, the treated horses were put into a variable interval response apparatus half an hour post Hordenine administration. There were no continuing stimulant or depressive effects observed.
- Oral administration of the same dose of Hordenine didn’t show any changes in the heart rate, breathing rate, basal body temperature, or behaviour of the horse.
Pharmacokinetics of Hordenine
- The concentration of Hordenine in the blood, post the intravenous dose, reached its peak at about 1.0 micrograms/ml and then started to decrease in a bi-exponential manner.
- The kinetics of the plasma concentration supported the concept of an open two-compartment system. The alpha-phase half-life was approximately 3 minutes, and the beta-phase half-life was around 35 minutes.
- The highest total urinary concentrations of Hordenine, including both free and conjugated forms, were found to be about 400 micrograms/ml. The concentration then fell exponentially, returning to normal levels 24 hours after the treatments.
Cite This Article
APA
Frank M, Weckman TJ, Wood T, Woods WE, Tai CL, Chang SL, Ewing A, Blake JW, Tobin T.
(1990).
Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse.
Equine Vet J, 22(6), 437-441.
https://doi.org/10.1111/j.2042-3306.1990.tb04312.x Publication
Researcher Affiliations
- Kentucky Equine Drug Research Program, Graduate Center in Toxicology, University of Kentucky, Lexington 40506.
MeSH Terms
- Administration, Oral
- Alkaloids / administration & dosage
- Alkaloids / pharmacokinetics
- Alkaloids / pharmacology
- Animals
- Behavior, Animal / drug effects
- Body Temperature / drug effects
- Female
- Heart Rate / drug effects
- Horses / metabolism
- Horses / physiology
- Injections, Intravenous / veterinary
- Respiration / drug effects
- Sympathomimetics / pharmacokinetics
- Sympathomimetics / pharmacology
- Tyramine / analogs & derivatives
Citations
This article has been cited 9 times.- Hahn M, Lindemann V, Behrens M, Mulac D, Langer K, Esselen M, Humpf HU. Permeability of dopamine D2 receptor agonist hordenine across the intestinal and blood-brain barrier in vitro. PLoS One 2022;17(6):e0269486.
- Anwar S, Mohammad T, Shamsi A, Queen A, Parveen S, Luqman S, Hasan GM, Alamry KA, Azum N, Asiri AM, Hassan MI. Discovery of Hordenine as a Potential Inhibitor of Pyruvate Dehydrogenase Kinase 3: Implication in Lung Cancer Therapy. Biomedicines 2020 May 14;8(5).
- Roeder L, Boonstra TW, Kerr GK. Corticomuscular control of walking in older people and people with Parkinson's disease. Sci Rep 2020 Feb 19;10(1):2980.
- Dinis-Oliveira RJ, Pereira CL, da Silva DD. Pharmacokinetic and Pharmacodynamic Aspects of Peyote and Mescaline: Clinical and Forensic Repercussions. Curr Mol Pharmacol 2019;12(3):184-194.
- Park H, Ha J, Koo JY, Park J, Park SB. Label-free target identification using in-gel fluorescence difference via thermal stability shift. Chem Sci 2017 Feb 1;8(2):1127-1133.
- Beury-Cirou A, Tannières M, Minard C, Soulère L, Rasamiravaka T, Dodd RH, Queneau Y, Dessaux Y, Guillou C, Vandeputte OM, Faure D. At a supra-physiological concentration, human sexual hormones act as quorum-sensing inhibitors. PLoS One 2013;8(12):e83564.
- Hoffman JR, Kang J, Ratamess NA, Rashti SL, Tranchina CP, Faigenbaum AD. Thermogenic effect of an acute ingestion of a weight loss supplement. J Int Soc Sports Nutr 2009 Jan 6;6:1.
- Pinckaers NET, Blankesteijn WM, Mircheva A, Shi X, Opperhuizen A, Schooten FV, Vrolijk MF. In Vitro Activation of Human Adrenergic Receptors and Trace Amine-Associated Receptor 1 by Phenethylamine Analogues Present in Food Supplements. Nutrients 2024 May 22;16(11).
- Doesburg-van Kleffens M, Zimmermann-Klemd AM, Gründemann C. An Overview on the Hallucinogenic Peyote and Its Alkaloid Mescaline: The Importance of Context, Ceremony and Culture. Molecules 2023 Dec 5;28(24).
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