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medetomidine

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Description

Medetomidine is an α2-adrenergic agonist with sedative, analgesic, and anesthetic properties. It is a highly selective and potent α2-receptor agonist with a long duration of action. It is synthesized through a series of chemical reactions involving a benzimidazole derivative and a chiral auxiliary. Medetomidine is used in veterinary medicine as a sedative, analgesic, and anesthetic agent for a variety of species, including dogs, cats, and horses. It is also used as a research tool to study the effects of α2-receptor activation in the central nervous system and other tissues. Medetomidine is being investigated for its potential therapeutic uses in humans, such as the treatment of pain, anxiety, and insomnia. Its effects are attributed to its ability to activate α2-adrenoceptors in the central nervous system, leading to inhibition of norepinephrine release and subsequent sedation, analgesia, and anxiolysis. Medetomidine's importance lies in its ability to provide safe and effective sedation and analgesia in both veterinary and research settings. The compound has a high affinity for α2-adrenoceptors, resulting in a strong and prolonged effect. The research on medetomidine focuses on understanding its pharmacological properties, therapeutic potential, and potential adverse effects. The study of this compound could lead to the development of new and improved medications for pain management, anxiety disorders, and other conditions.'

Medetomidine: An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68602
CHEMBL ID77921
CHEBI ID48552
SCHEMBL ID26432
MeSH IDM0140434

Synonyms (63)

Synonym
CHEMBL77921 ,
bdbm50036913
HY-17034
BRD-A66563878-003-01-8
medetomidine
6918-06-5
(rs)-4-(alpha,2,3-trimethylbenzyl)imidazol
medetomidinum [latin]
1h-imidazole, 4-(1-(2,3-dimethylphenyl)ethyl)-
medetomidina [spanish]
medetomidine [inn:ban]
ih-imidazole, 4(1-(2,3-dimethylphenyl)ethyl)-
medetomidina
4-[1-(2,3-dimethylphenyl)ethyl]-1h-imidazole
CHEBI:48552 ,
(+-)-4-(alpha,2,3-trimethylbenzyl)imidazole
86347-14-0
medetomidinum
L001361
L000223
5-[1-(2,3-dimethylphenyl)ethyl]-1h-imidazole
domitor [veterinary] (tn)
D08165
medetomidine (inn)
FT-0666307
AKOS016010776
mr15e85mqm ,
unii-mr15e85mqm
FT-0670775
CS-0734
1h-imidazole, 4-(1-(2,3-dimethylphenyl)ethyl)-, (+/-)-
medetomidine [inn]
medetomidine [green book]
(+/-)-4-(.alpha.,2,3-trimethylbenzyl)imidazole
medetomidine [mi]
SCHEMBL26432
DTXSID6048258 ,
1h-imidazole, 4-[1-(2,3-dimethylphenyl)ethyl]-
4-(1-(2,3-dimethylphenyl)ethyl)-1h-imidazole
AB01566810_01
(s)-medetomidine; dexmedetomidinum
HMS3651H20
mfcd24392996
4-[(r)-1-(2,3-dimethylphenyl)ethyl]-1h-imidazole
domtor
BCP06913
Q427179
SY116126
FT-0716677
DB11428
(+/-)-4-(alpha,2,3-trimethylbenzyl)imidazole
AS-35172
(rs)-4-[1-(2,3-dimethylphenyl)ethyl]-3h-imidazole
BCP12592
SB17478
AKOS037643760
mfcd00864346
SY114102
A863235
EN300-7382825
medetomidinum (latin)
dtxcid1028233
domitor (veterinary)

Research Excerpts

Overview

Medetomidine is an alpha(2)-adrenoceptor agonist with sedative and analgesic properties. It is a relatively new sedative analgesic drug that is approved for use in dogs in Canada.

ExcerptReferenceRelevance
"Medetomidine is an alpha(2)-adrenoceptor agonist with sedative and analgesic properties. "( Differences in hepatic cytochrome P450 activity correlate with the strain-specific biotransformation of medetomidine in AX/JU and IIIVO/JU inbred rabbits.
Avsaroglu, H; Bergwerff, AA; Bull, S; Fink-Gremmels, J; Hellebrekers, LJ; Maas-Bakker, RF; Scherpenisse, P; Van Lith, HA; Van Zutphen, LF, 2008
)
2
"Medetomidine is a potent and selective alpha2-adrenergic agonist. "( Metabolic stability and determination of cytochrome P450 isoenzymes' contribution to the metabolism of medetomidine in dog liver microsomes.
Beaudry, F; Duhamel, MC; Troncy, E, 2010
)
2.02
"Medetomidine is a new antifouling agent, and its effects in non-target aquatic organisms have been investigated. "( Colour and melanophore function in rainbow trout after long term exposure to the new antifoulant medetomidine.
Förlin, L; Hedberg, D; Kristiansson, E; Lennquist, A; Mårtensson Lindblad, LG, 2010
)
2.02
"Medetomidine is a new antifouling substance, highly effective against barnacles. "( Short-term effects of medetomidine on photosynthesis and protein synthesis in periphyton, epipsammon and plankton communities in relation to predicted environmental concentrations.
Blanck, H; Eriksson, KM; Ohlauson, C, 2012
)
2.14
"Medetomidine is a relatively new sedative analgesic drug that is approved for use in dogs in Canada. "( A review of the physiological effects of alpha2-agonists related to the clinical use of medetomidine in small animal practice.
Sinclair, MD, 2003
)
1.98
"Medetomidine is a commonly used sedative in veterinary medicine whether administered alone or in combination with an opioid such as butorphanol. "( Effects of medetomidine and medetomidine-butorphanol combination on Schirmer tear test 1 readings in dogs.
Mellor, D; Mould, J; Sanchez, RF,
)
1.96
"Medetomidine may prove to be a useful adjunct to peripheral nerve blockade with local anesthetics."( The effects of medetomidine on radial nerve blockade with mepivacaine in dogs.
Lamont, LA; Lemke, KA, 2008
)
2.14
"Medetomidine is a chiral imidazole derivate whose dextroenantiomer is pharmacologically active. "( Regio- and stereospecific N-glucuronidation of medetomidine: the differences between UDP glucuronosyltransferase (UGT) 1A4 and UGT2B10 account for the complex kinetics of human liver microsomes.
Aitio, O; Finel, M; Kaivosaari, S; Koskinen, M; Salonen, JS; Sipilä, J; Toivonen, P, 2008
)
2.05
"Dexmedetomidine is a new alpha 2 adrenergic agonist anaesthetic adjuvant. "( Dexmedetomidine does not modify the neuromuscular blocking action of vecuronium in the anaesthetized rat.
Henry, AF; Partridge, BL; Weinger, MB, 1995
)
1.53
"Dexmedetomidine is a new potent and highly selective alpha 2-adrenoceptor agonist with sedative-hypnotic and anesthetic sparing properties. "( Dexmedetomidine premedication attenuates ketamine-induced cardiostimulatory effects and postanesthetic delirium.
Levänen, J; Mäkelä, ML; Scheinin, H, 1995
)
1.53
"Dexmedetomidine is an effective premedication before i.v. "( Dexmedetomidine premedication before intravenous regional anesthesia in minor outpatient hand surgery.
Jaakola, ML,
)
1.37
"Dexmedetomidine is a novel alpha 2-adrenoceptor agonist that may provide beneficial effects as premedication for anesthesia. "( Pharmacokinetics and pharmacodynamics of transdermal dexmedetomidine.
Kallio, A; Kivistö, KT; Neuvonen, PJ, 1994
)
1.16
"Dexmedetomidine (DEX) is a highly selective alpha 2 agonist with marked sedative and analgesic properties thought to be mediated via reduction of central noradrenergic transmission. "( Dexmedetomidine decreases seizure threshold in a rat model of experimental generalized epilepsy.
McPherson, RW; Mirski, MA; Rossell, LA; Traystman, RJ, 1994
)
1.53
"Dexmedetomidine is an alpha 2 agonist with potential utility in clinical anesthesia for both its sedative and sympatholytic properties."( The pharmacokinetics and hemodynamic effects of intravenous and intramuscular dexmedetomidine hydrochloride in adult human volunteers.
Dyck, JB; Haack, C; Maze, M; Shafer, SL; Vuorilehto, L, 1993
)
1.13
"Dexmedetomidine is a selective alpha 2-adrenoceptor agonist which has previously been shown to reduce the ocular pressure of normotensive rabbits as well as those with pressures artificially elevated by laser irradiation. "( Systemic absorption and systemic effects of ocularly administered dexmedetomidine in rabbits.
Jäsberg, K; MacDonald, E; Salonen, JS; Urtti, A; Vartiainen, J; Vuorilehto, L, 1993
)
1.14
"Dexmedetomidine is a new potent and selective alpha 2-agonist that might prove useful as a preanesthetic agent."( Intramuscular dexmedetomidine as premedication for general anesthesia. A comparative multicenter study.
Ali-Melkkilä, T; Jaakola, ML; Kanto, J; Kaukinen, S; Scheinin, H; Sjövall, S; Turunen, J, 1993
)
1.25
"Medetomidine is a relatively new sedative analgesic in dogs and cats but some precautions are required when using it. "( Medetomidine sedation in dogs and cats: a review of its pharmacology, antagonism and dose.
Cullen, LK, 1996
)
3.18
"Dexmedetomidine (Dex) is an alpha 2-adrenergic agonist that decreases cerebral blood flow (CBF) when administered systemically. "( Pial arteriolar constriction to alpha 2-adrenergic agonist dexmedetomidine in the rat.
Asano, Y; Kawaguchi, T; Koehler, RC; McPherson, RW, 1997
)
1.16
"Dexmedetomidine is a selective alpha2-adrenoceptor agonist with centrally mediated sympatholytic, sedative, and analgesic effects. "( Postoperative pharmacokinetics and sympatholytic effects of dexmedetomidine.
Fisher, DM; Richardson, CA; Scheinin, M; Talke, P, 1997
)
1.16
"Levomedetomidine, which is a weak agonist in some test systems, reduced intracellular Ca2+ levels and further increased forskolin-stimulated cAMP production and therefore can be classified as an inverse agonist."( Protean agonism at alpha2A-adrenoceptors.
Akerman, KE; Cockcroft, V; Huifang, G; Jansson, CC; Kukkonen, JP; Näsman, J; Savola, JM; Virtanen, R; Wurster, S, 1998
)
0.78
"Medetomidine is an alpha-2 adrenoceptor agonist widely used in dogs, producing sedation, analgesia and cardiovascular depression. "( Hemodynamic effects of medetomidine in the dog: a dose titration study.
Pypendop, BH; Verstegen, JP,
)
1.88
"Medetomidine is a selective, specific, and potent alpha2-adrenergic receptor agonist that has been utilized successfully as a sedative/analgesic agent in a variety of domestic and nondomestic animals. "( Cardiovascular, respiratory, thermoregulatory, sedative, and analgesic effects of intravenous administration of medetomidine in rhesus macaques (Macaca mulatta).
Capuano, SV; Lerche, NW; Valverde, CR, 1999
)
1.96
"Medetomidine is a safe and reliable alternative to manual restraint in cassowaries."( Use of medetomidine for capture and restraint of cassowaries (Casuarius casuaris).
Reid, KE; Westcott, DA, 2002
)
2.21
"Dexmedetomidine (DMED) is a novel alpha 2 adrenergic agonist that has been shown to have potent analgesic and anesthetic sparing effects. "( Ventilatory effects of dexmedetomidine, atipamezole, and isoflurane in dogs.
Abdul-Rasool, I; Bloor, B; Hadlock, S; Hsieh, J; Kobayashi, D; Nguyen, D; Singer, F; Ward, D, 1992
)
1.21
"Dexmedetomidine is an extremely potent alpha 2 adrenoceptor agonist which can reduce anaesthetic requirements by up to 90%. "( Dexmedetomidine, a potent and highly specific alpha 2 agonist, evokes cytosolic calcium surge in astrocytes but not in neurons.
Code, WE; Hertz, L; Zhao, Z, 1992
)
1.53
"Dexmedetomidine (DMED) is a highly selective centrally acting alpha 2-adrenergic agonist thought to provide significant sedation without appreciable ventilatory effects. "( Effects of intravenous dexmedetomidine in humans. I. Sedation, ventilation, and metabolic rate.
Belleville, JP; Bloor, BC; Maze, M; Ward, DS, 1992
)
1.21
"Medetomidine (MED) is a novel, selective, alpha 2 adrenergic agonist with potent sedative, hypnotic, and analgesic properties, currently undergoing evaluation as an anesthetic adjuvant. "( Ketamine as a probe for medetomidine stereoisomer inhibition of human liver microsomal drug metabolism.
Herrmann, S; Kharasch, ED; Labroo, R, 1992
)
2.03
"Dexmedetomidine (DMED) is a novel clonidine-like compound known to have sedative, analgesic, and cardiovascular stabilizing qualities. "( Effects of intravenous dexmedetomidine in humans. II. Hemodynamic changes.
Belleville, JP; Bloor, BC; Maze, M; Ward, DS, 1992
)
1.21
"Dexmedetomidine is a highly selective alpha 2-adrenoceptor agonist. "( Antinociceptive properties of intrathecal dexmedetomidine in rats.
Fisher, B; Peterson, BM; Yaksh, TL; Zornow, MH, 1991
)
1.16
"Dexmedetomidine is an alpha 2-adrenergic agonist that decreases central sympathetic activity and reduces the anesthetic requirement for halothane. "( Dexmedetomidine improves neurologic outcome from incomplete ischemia in the rat. Reversal by the alpha 2-adrenergic antagonist atipamezole.
Albrecht, RF; Hoffman, WE; Kochs, E; Thomas, C; Werner, C, 1991
)
1.52
"Medetomidine (MED) is a veterinary sedative whose mode of action is activation of alpha-2 adrenoceptors. "( Comparison of the behavioral and neurochemical effects of the two optical enantiomers of medetomidine, a selective alpha-2-adrenoceptor agonist.
MacDonald, E; Scheinin, H; Scheinin, M; Virtanen, R, 1991
)
1.95
"Dexmedetomidine is a potentially useful tool for studies of the physiology and pharmacology of alpha 2-adrenoceptors in human beings and may have therapeutic applications in clinical conditions in which sedative and sympatholytic effects are considered beneficial, such as premedication for anesthesia and surgery."( Effects of dexmedetomidine, a selective alpha 2-adrenoceptor agonist, on hemodynamic control mechanisms.
Kallio, A; Koulu, M; Ponkilainen, R; Ruskoaho, H; Scheinin, H; Scheinin, M; Viinamäki, O, 1989
)
1.15
"Medetomidine appears to be a potent sedative and analgesic agent for clinical use."( The clinical efficacy of medetomidine.
Vähä-Vahe, T, 1989
)
1.3
"Medetomidine is a sedative and analgesic drug intended for use in dogs and cats but it can also be successfully used in many other species. "( Introduction to the clinical pharmacology of medetomidine.
Vainio, O, 1989
)
1.98

Effects

Medetomidine is a popular choice for anesthetizing rats during long-lasting sessions of blood-oxygen-level dependent (BOLD) functional magnetic resonance imaging (fMRI) It has been authorized in ship hull paints as an antifouling biocide under the biocidal product regulation in Europe.

ExcerptReferenceRelevance
"Medetomidine has become a popular choice for anesthetizing rats during long-lasting sessions of blood-oxygen-level dependent (BOLD) functional magnetic resonance imaging (fMRI). "( Temporal stability of fMRI in medetomidine-anesthetized rats.
Baudewig, J; Boretius, S; Sirmpilatze, N, 2019
)
2.25
"Medetomidine has been authorized in ship hull paints as an antifouling biocide under the biocidal product regulation in Europe since 2016. "( Photochemical fate of medetomidine in coastal and marine environments.
Apell, JN; Bollmann, UE; Cai, Y; McNeill, K; Pflug, NC, 2021
)
2.38
"Medetomidine has been reported as a reliable, repeatable and reversible immobilisation agent in small estuarine crocodilians."( Medetomidine immobilisation and atipamezole reversal in large estuarine crocodiles (Crocodylus porosus) using metabolically scaled dosages.
Olsson, A; Phalen, D, 2012
)
2.54
"Dexmedetomidine (DM) has been found to depress cardiac function in dogs, even after autonomic denervation."( Effects of dexmedetomidine on systemic and coronary hemodynamics in the anesthetized dog.
Bloor, BC; Flacke, JW; Flacke, WE; McIntee, DF; Sagan, M, 1993
)
1.16
"L-medetomidine, which has no sedative/hypnotic effect, did not decrease cGMP."( Alpha-2 adrenoceptor agonists decrease cyclic guanosine 3',5'-monophosphate in the mouse brain.
Shen, H; Virag, L; Vulliemoz, Y, 1996
)
0.85
"Medetomidine has been shown to produce a reliable state of sedation, relaxation and recumbency suitable for small animal practice."( The clinical efficacy of medetomidine.
Vähä-Vahe, T, 1989
)
1.3

Actions

Dexmedetomidine appears at a lower dose than its antinociceptive effect. The lower dose of atipamezole (0.1 mg/kg) did not significantly alter the evoked overflow of amino acids.

ExcerptReferenceRelevance
"dexmedetomidine appears at a lower dose than its antinociceptive effect."( Mydriatic and antinociceptive effects of intrathecal dexmedetomidine in conscious rats.
Benedek, G; Horváth, G; Kovács, M; Szikszay, M, 1994
)
1.05
"Dexmedetomidine and the lower dose of atipamezole (0.1 mg/kg) did not significantly alter the evoked overflow of amino acids."( Effect of alpha 2-adrenergic drugs dexmedetomidine and atipamezole on extracellular amino acid levels in vivo.
Haapalinna, A; Halonen, T; Riekkinen, P; Valtonen, P, 1995
)
1.08

Treatment

Dexmedetomidine-treated rats had lower plasma catecholamines (20% of control) and larger decreases in CBF during ischemia compared with controls. Cats treated with medetOMidine or medetomazine and midazolam in combination with alfaxalone had lower concentrations of nonesterified fatty acids during anesthesia.

ExcerptReferenceRelevance
"Dexmedetomidine-treated rats had lower plasma catecholamines (20% of control) and larger decreases in CBF during ischemia compared with controls."( Interaction of catecholamines and nitrous oxide ventilation during incomplete brain ischemia in rats.
Albrecht, RF; Baughman, VL; Hoffman, WE, 1993
)
0.8
"Medetomidine-treated animals had a decreased respiratory rate, longer duration of analgesic effect, increased incidence of bradycardia, vomiting and twitching, were less noise responsive and shivered less throughout the study."( Comparison of medetomidine and fentanyl-droperidol in dogs: sedation, analgesia, arterial blood gases and lactate levels.
Dyson, DH; Pettifer, GR, 1993
)
1.37
"Dexmedetomidine pretreatment augmented the actions of halothane on arterial pressure, heart rate, and the EEG."( Pretreatment with dexmedetomidine: altered indices of anesthetic depth for halothane in the neuraxis of cats.
Drexler, C; Farber, NE; Ganjoo, P; Schmeling, WT; Staunton, M, 1999
)
1.14
"In medetomidine-treated dogs, heart rate was significantly lower than in controls, and blood pressure did not change significantly from baseline. "( Cardiorespiratory responses and plasma cortisol concentrations in dogs treated with medetomidine before undergoing ovariohysterectomy.
Fox, SM; Ko, JC; Lange, DN; Mandsager, RE, 2000
)
1.15
"Cats treated with medetomidine or medetomidine and midazolam in combination with alfaxalone, compared with alfaxalone alone, had lower concentrations of nonesterified fatty acids during anesthesia."( A randomized clinical trial on effects of alfaxalone combined with medetomidine and midazolam in preventing stress-related neurohormonal and metabolic responses of isoflurane-anesthetized cats undergoing surgery.
Hikasa, Y; Kamohara, H; Kamohara, T, 2022
)
1.28
"Treatment with medetomidine-midazolam resulted in a shorter and smoother induction, compared with acepromazine-butorphanol or midazolam-butorphanol treatment, whereas the cardiovascular changes were greater."( Effects of medetomidine-midazolam, midazolambutorphanol, or acepromazine-butorphanol as premedicants for mask induction of anesthesia with sevoflurane in dogs.
Mutoh, T; Nishimura, R; Sasaki, N, 2002
)
1.04
"In treated dogs, medetomidine was administered (time, 0 minutes); midazolam and butorphanol were administered when effects of medetomidine were maximal (time, 20), and atipamezole was administered subsequently (time 60). "( Cardiorespiratory effects of a combination of medetomidine, midazolam, and butorphanol in dogs.
Pypendop, B; Verstegen, J, 1999
)
0.9

Toxicity

There were few adverse side effects, but they included prolonged sedation, hypothermia, apnoea and bradycardia. No adverse effects were observed after the administration of atipamezole, which effectively reversed all the clinical effects.

ExcerptReferenceRelevance
" Sixteen of the dogs suffered an adverse effect, 13 of them vomited."( Clinical efficacy and safety of propofol or ketamine anaesthesia in dogs premedicated with medetomidine.
Hellebrekers, LJ; Hird, JF; Rosenhagen, CU; Sap, R; Vainio, O; van Herpen, H, 1998
)
0.52
" In the present study, the alpha2-adrenergic agonists xylazine and medetomidine were combined with tribromoethanol to examine their use as alternate and safe anesthetic regimes in rats."( Tribromoethanol-medetomidine combination provides a safe and reversible anesthetic effect in Sprague-Dawley rats.
Bay, TN; Brown, SR; Gopalan, C; Hegade, GM; Talcott, MR, 2005
)
0.91
" The reporting of adverse events was low and the most commonly observed event was vomiting (7%)."( Evaluation of the clinical efficacy and safety of dexmedetomidine or medetomidine in cats and their reversal with atipamezole.
Aspegrén, JC; Granholm, M; McKusick, BC; Westerholm, FC, 2006
)
0.58
" There were few adverse side effects, but they included prolonged sedation, hypothermia, apnoea and bradycardia; no adverse effects were observed after the administration of atipamezole, which effectively reversed all the clinical effects of dexmedetomidine and medetomidine."( Evaluation of the clinical efficacy and safety of intramuscular and intravenous doses of dexmedetomidine and medetomidine in dogs and their reversal with atipamezole.
Aspegrén, JC; Granholm, M; McKusick, BC; Westerholm, FC, 2007
)
0.74
" Overall, midazolam-ketamine provided safe and effective sedation for catheterization and intubation of both healthy and CI pigs."( Effective and safe anesthesia for Yorkshire and Yucatan swine with and without cardiovascular injury and intervention.
Abusakran-Monday, KA; Burkholder, TH; Foltz, CJ; Linkenhoker, JR; Linton, CG; Rosero, AP; Walden, A, 2010
)
0.36
" The depth of anaesthesia was sufficient to allow safe removal of the animals from the enclosure, intravenous catheter placement and manipulation; however, the anaesthetic effect was short-acting (20 (±7) minutes in orangutans, 16 (±14) in gorillas, and 10 (±4) minutes in chimpanzees, respectively) and isoflurane administration was necessary in the majority of the apes to prolong the duration of anaesthesia, especially when lengthier procedures were performed."( Evaluation of effectiveness, safety and reliability of intramuscular medetomidine-ketamine for captive great apes.
Adami, C; Bergadano, A; Hoby, S; Wenker, C, 2012
)
0.61
" No adverse effects were observed after recovery from anesthesia."( EFFICACY AND SAFETY OF A MEDETOMIDINE-AZAPERONE-ALFAXALONE COMBINATION IN CAPTIVE WHITE-TAILED DEER (ODOCOILEUS VIRGINIANUS).
Caulkett, N; Pon, K; Woodbury, M, 2016
)
0.74

Pharmacokinetics

The only statistically significant effects of medetomidine on the pharmacokinetics of atipamezole in this study were the slight decrease of Cl and Cmax as well as the increase of AUC. There was no difference in estimated thiopental effect site concentrations between dexmedetmidine and control patients, suggesting the absence of a major pharmacodynamic interaction.

ExcerptReferenceRelevance
" The pharmacodynamic effects of medetomidine, a novel alpha 2-adrenoceptor agonist, are reviewed."( Medetomidine--a novel alpha 2-adrenoceptor agonist: a review of its pharmacodynamic effects.
Lammintausta, R; MacDonald, E; Scheinin, H; Scheinin, M; Virtanen, R, 1989
)
2
" In plasma/serum a distribution phase with a half-life of only a few minutes was observed."( Pharmacokinetics of medetomidine.
Salonen, JS, 1989
)
0.6
" Furthermore, the pharmacodynamic action of alpha-2 adrenergic agonists, like many other sedative hypnotics (e."( Alpha-2 adrenergic modulation of sleep: time-of-day-dependent pharmacodynamic profiles of dexmedetomidine and clonidine in the rat.
Dement, WC; Edgar, DM; Maze, M; Seidel, WF, 1995
)
0.51
" There was no difference in estimated thiopental effect site concentrations between dexmedetomidine and control patients, suggesting the absence of a major pharmacodynamic interaction."( Dexmedetomidine decreases thiopental dose requirement and alters distribution pharmacokinetics.
Bührer, M; Lauber, R; Maitre, PO; Mappes, A; Stanski, DR, 1994
)
1.13
"The thiopental dose-sparing effect of dexmedetomidine on the electroencephalogram is not the result of a pharmacodynamic interaction but rather can be explained by a dexmedetomidine-induced decrease in thiopental distribution volume and distribution clearances."( Dexmedetomidine decreases thiopental dose requirement and alters distribution pharmacokinetics.
Bührer, M; Lauber, R; Maitre, PO; Mappes, A; Stanski, DR, 1994
)
1.18
" For opioids, relative analgesic potency of epidural to intravenous administration decreases with increasing lipophilicity, but such pharmacodynamic studies have been performed with only one alpha 2-adrenergic agonist, clonidine, of moderate lipophilicity."( Pharmacokinetics and pharmacodynamics of intraspinal dexmedetomidine in sheep.
Bucklin, BA; Eisenach, JC; Jackson, C; Kallio, A; Shafer, SL, 1994
)
0.53
" Dexmedetomidine absorption in CSF after epidural injection was rapid (Tmax = 5-20 min), although pharmacokinetic modeling suggested a biphasic absorption process."( Pharmacokinetics and pharmacodynamics of intraspinal dexmedetomidine in sheep.
Bucklin, BA; Eisenach, JC; Jackson, C; Kallio, A; Shafer, SL, 1994
)
1.09
" The only statistically significant effects of medetomidine on the pharmacokinetics of atipamezole in this study were the slight decrease of Cl and Cmax as well as the increase of AUC."( Atipamezole increases medetomidine clearance in the dog: an agonist-antagonist interaction.
Anttila, M; Salonen, S; Vainio, O; Vuorilehto, L, 1995
)
0.86
" We conclude that infusion of dexmedetomidine by CCIP using published pharmacokinetic parameters overshoots target dexmedetomidine concentrations during the early postoperative period."( Postoperative pharmacokinetics and sympatholytic effects of dexmedetomidine.
Fisher, DM; Richardson, CA; Scheinin, M; Talke, P, 1997
)
0.82
"We studied the pharmacokinetic and sympatholytic effects of dexmedetomidine during the immediate postoperative period and found that during this period, the published pharmacokinetic data slightly overshoot target plasma dexmedetomidine concentrations."( Postoperative pharmacokinetics and sympatholytic effects of dexmedetomidine.
Fisher, DM; Richardson, CA; Scheinin, M; Talke, P, 1997
)
0.78
" Other pharmacokinetic parameters of medetomidine were not significantly altered by atipamezole."( Pharmacokinetics of medetomidine and atipamezole in dairy calves: an agonist-antagonist interaction.
Arnemo, JM; Horsberg, TE; Ranheim, B; Ryeng, KA; Søli, NE, 1998
)
0.9
" Medetomidine concentrations were determined by liquid chromatography-Mass Spectrometry and used for calculation of pharmacokinetic parameters using noncompartmental and compartmental analysis."( Pharmacokinetics and pharmacodynamics of intravenous medetomidine in the horse.
Grimsrud, KN; Mama, KR; Stanley, SD; Steffey, EP, 2012
)
1.54
" The elimination half-life was 29."( Pharmacokinetics and pharmacodynamics of intravenous medetomidine in the horse.
Grimsrud, KN; Mama, KR; Stanley, SD; Steffey, EP, 2012
)
0.63
"Behavioral and physiological effects following intravenous administration positively correlate with pharmacokinetic profiles from plasma medetomidine concentrations."( Pharmacokinetics and pharmacodynamics of intravenous medetomidine in the horse.
Grimsrud, KN; Mama, KR; Stanley, SD; Steffey, EP, 2012
)
0.83
"The present study characterizes the pharmacokinetic (PK) and pharmacodynamic (PD) relationships of the α2-adrenergic receptor agonists detomidine (DET), medetomidine (MED) and dexmedetomidine (DEX) in parallel groups of horses from in vivo data after single bolus doses."( Pharmacokinetic and pharmacodynamic analysis comparing diverse effects of detomidine, medetomidine, and dexmedetomidine in the horse: a population analysis.
Ait-Oudhia, S; Durbin-Johnson, BP; Grimsrud, KN; Jusko, WJ; Mama, KR; Rezende, ML; Rocke, DM; Stanley, SD, 2015
)
0.84
" The AUC (6 hours ng mL(-1)) and CMAX (6 ng mL(-1)) of methadone significantly increased to 541 hours ng mL(-1) and 47."( Chloramphenicol significantly affects the pharmacokinetics of oral methadone in Greyhound dogs.
KuKanich, B; KuKanich, K, 2015
)
0.42
" Antagonism by MK-467 of medetomidine-evoked vasoconstriction is seen as the mechanism behind this pharmacokinetic drug interaction."( Effects of MK-467 on the antinociceptive and sedative actions and pharmacokinetics of medetomidine in dogs.
Bennett, RC; Hänninen, L; Raekallio, MR; Rinne, VM; Salla, KM; Scheinin, M; Vainio, OM, 2016
)
0.96
" Plasma alfaxalone concentrations were quantified by a liquid chromatography tandem-mass spectrometry method and analysed by non-compartmental pharmacokinetic analysis."( Clinical pharmacokinetics and pharmacodynamics of intravenous alfaxalone in young Thoroughbred horses premedicated with medetomidine and midazolam.
Aoki, M; Kushiro, A; Mae, N; Maeda, T; Minamijima, Y; Nagata, SI; Ohta, M; Wakuno, A; Yamazaki, Y, 2019
)
0.72
"To assess the differences in the pharmacokinetic profiles of S-ketamine, R-ketamine and their metabolites, S-norketamine and R-norketamine, and to measure relevant physiologic variables after intravenous administration of racemic (RS) ketamine or S-ketamine alone in Beagle dogs sedated with medetomidine."( Pharmacokinetics of S-ketamine and R-ketamine and their active metabolites after racemic ketamine or S-ketamine intravenous administration in dogs sedated with medetomidine.
Barbarossa, A; Bektas, RN; Bettschart-Wolfensberger, R; Hartnack, S; Kutter, APN; Romagnoli, N; Roncada, P, 2020
)
0.93
"S-ketamine showed a two-compartment kinetic profile; no statistically significant differences were observed between its concentrations or in the calculated pharmacokinetic parameters following S- or RS-ketamine."( Pharmacokinetics of S-ketamine and R-ketamine and their active metabolites after racemic ketamine or S-ketamine intravenous administration in dogs sedated with medetomidine.
Barbarossa, A; Bektas, RN; Bettschart-Wolfensberger, R; Hartnack, S; Kutter, APN; Romagnoli, N; Roncada, P, 2020
)
0.75
"The goal of this study was to investigate the pharmacokinetic (PK) behaviour of dexmedetomidine in dogs administered as a pure enantiomer versus as part of a racemic mixture."( Enantiospecific pharmacokinetics of intravenous dexmedetomidine in beagles.
Barbarossa, A; Bardhi, A; Forss Pleyers, T; Guidi, M; Levionnois, OL; Raillard, M; Siegenthaler, J; Spadavecchia, C, 2022
)
1.2
"7 ml/min/kg, the mean terminal half-life was 82."( Pharmacokinetics of intravenous propofol in southern white rhinoceros (Ceratotherium simum simum) after intramuscular etorphine-butorphanol-medetomidine-azaperone.
Berlin, ER; Clancy, MM; Ferris, RL; Howard, LL; Kinney, ME; Knych, HK; Mama, KR; Perrin, KL; Phair, KA, 2023
)
1.11
"This study provides pharmacokinetic data and insight into the effects of propofol in rhinoceros anesthetized using etorphine, butorphanol, medetomidine, and azaperone."( Pharmacokinetics of intravenous propofol in southern white rhinoceros (Ceratotherium simum simum) after intramuscular etorphine-butorphanol-medetomidine-azaperone.
Berlin, ER; Clancy, MM; Ferris, RL; Howard, LL; Kinney, ME; Knych, HK; Mama, KR; Perrin, KL; Phair, KA, 2023
)
1.31

Compound-Compound Interactions

The time course of the effects of ethanol alone and in combination with the selective alpha 2-adrenoceptor agonist dexmedetomidine and atipamezole was studied in NIH-Swiss mice. Sevoflurane requirement, cardiovascular function, and induction/recovery quality were compared between horses maintained with sevof lurane and those maintained with alfaxalone.

ExcerptReferenceRelevance
"The time course of the effects of ethanol alone and in combination with the selective alpha 2-adrenoceptor agonist dexmedetomidine and the alpha-adrenoceptor antagonist atipamezole was studied in NIH-Swiss mice."( The effects of ethanol in combination with the alpha 2-adrenoceptor agonist dexmedetomidine and the alpha 2-adrenoceptor antagonist atipamezole on brain monoamine metabolites and motor performance of mice.
Björn, M; Idänpään-Heikkilä, JJ; Seppälä, T, 1995
)
0.73
"Fifteen cats had anaesthesia induced by intramuscular injection of medetomidine combined with ketamine."( Cardiovascular changes associated with anaesthesia induced by medetomidine combined with ketamine in cats.
Dobromylskyj, P, 1996
)
0.77
"To evaluate effects of infusion of guaifenesin, ketamine, and medetomidine in combination with inhalation of sevoflurane versus inhalation of sevoflurane alone for anesthesia of horses."( Infusion of guaifenesin, ketamine, and medetomidine in combination with inhalation of sevoflurane versus inhalation of sevoflurane alone for anesthesia of horses.
Abrahamsen, E; Izumisawa, Y; Kotani, T; Lerch, P; Muir, WW; Tsubakishita, S; Yamashita, K, 2002
)
0.82
"The study was conducted in 9 healthy adult goats of either sex, weighing 15-20 kg, to evaluate and compare the clinicophysiological effects of spinally administered ketamine alone and in combination with xylazine and medetomidine."( Clinicophysiological effects of spinally administered ketamine and its combination with xylazine and medetomidine in healthy goats.
Aithal, HP; Kinjavdekar, P; Pawde, AM; Singh, GR, 2007
)
0.74
" The purpose of this study was to identify the effects of daily serial sedation using ketamine (K) or ketamine combined with medetomidine (KM)."( The effect of daily repeated sedation using ketamine or ketamine combined with medetomidine on physiology and anesthetic characteristics in rhesus macaques.
Lugo-Roman, LA; Rico, PJ; Settle, TL, 2010
)
0.79
" This study aimed to compare the onset and depth of anaesthesia, and changes in vital signs, after intraperitoneal (IP) or subcutaneous (SC) administration of ketamine (75 mg kg(-1)) combined with medetomidine (1 mg kg(-1)) or dexmedetomidine (0."( A comparison of medetomidine and its active enantiomer dexmedetomidine when administered with ketamine in mice.
Burnside, WM; Cameron, AI; Flecknell, PA; Thomas, AA, 2013
)
0.92
"This study failed to demonstrate clinical advantages of the enantiomer dexmedetomidine over medetomidine when combined with ketamine to produce general anaesthesia in mice."( A comparison of medetomidine and its active enantiomer dexmedetomidine when administered with ketamine in mice.
Burnside, WM; Cameron, AI; Flecknell, PA; Thomas, AA, 2013
)
0.97
" Morphine at 1 or 2 mg/kg combined with medetomidine and alfaxalone in rabbits produced a suitable level of anaesthesia, although profound cardiorespiratory depression was found."( Cardiorespiratory, anaesthetic and recovery effects of morphine combined with medetomidine and alfaxalone in rabbits.
Del Mar Granados, M; Fernández-Sarmiento, A; Gómez-Villamandos, RJ; López Villalba, I; Manuel Domínguez, J; Morgaz, J; Muñoz-Rascón, P; Navarrete-Calvo, R, 2014
)
0.9
" Alfaxalone, alone or in combination with tramadol, did not produce satisfactory results for use as an anaesthetic for this species."( Anaesthetic effects in the ferret of alfaxalone alone and in combination with medetomidine or tramadol: a pilot study.
García-Olmo, DC; Giral, M; Gómez de Segura, IA; Gómez-Juárez, M, 2014
)
0.63
"The aim of the study was to evaluate the tolerability, sedative and analgesic effects of methadone in combination with medetomidine for premedication prior to neutering in healthy cats."( Methadone in combination with medetomidine as premedication prior to ovariohysterectomy and castration in the cat.
Bortolami, E; Murrell, JC; Slingsby, LS, 2015
)
0.91
"Medetomidine combined with methadone for premedication prior to neutering in healthy cats provided adequate analgesia for the first 6 h after administration with no adverse effects; effects overall were comparable with medetomidine combined with buprenorphine or butorphanol."( Methadone in combination with medetomidine as premedication prior to ovariohysterectomy and castration in the cat.
Bortolami, E; Murrell, JC; Slingsby, LS, 2015
)
2.15
"To compare the sedative effects of an intramuscular (IM) low dose of medetomidine in combination with butorphanol or methadone in dogs."( The sedative effects of intramuscular low-dose medetomidine in combination with butorphanol or methadone in dogs.
Canfrán, S; Costa-Farré, C; Gómez de Segura, IA; Puighibet, Z; Santos, L, 2015
)
0.91
"The pharmacological effects of intramuscular (IM) administration of alfaxalone combined with medetomidine and butorphanol were evaluated in 6 healthy beagle dogs."( The pharmacological effects of intramuscular administration of alfaxalone combined with medetomidine and butorphanol in dogs.
Fukui, S; Hatakeyama, N; Ishizuka, T; Itami, T; Miyoshi, K; Pasloske, K; Sano, T; Tamura, J; Yamashita, K, 2016
)
0.88
" Solutions containing mixtures of methadone combined with acepromazine, medetomidine or xylazine were stored in syringes at 25°C/60%RH."( Chemical stability of morphine and methadone, and of methadone in combination with acepromazine, medetomidine or xylazine, during prolonged storage in syringes.
Lee, DY; Watson, N; Whittem, T, 2017
)
0.91
" When in combination with acepromazine or xylazine, methadone also remained chemically stable, but the combination with medetomidine failed stability criteria prior to 6 months."( Chemical stability of morphine and methadone, and of methadone in combination with acepromazine, medetomidine or xylazine, during prolonged storage in syringes.
Lee, DY; Watson, N; Whittem, T, 2017
)
0.88
" PROCEDURES In a randomized crossover study, each dog received 5 premedication protocols (medetomidine [10 μg/kg, IV] alone [MED] and in combination with MK-467 at doses of 50 [MMK50], 100 [MMK100], and 150 [MMK150] μg/kg and 15 minutes after glycopyrrolate [10 μg/kg, SC; MGP]), with at least 14 days between treatments."( Cardiovascular effects of premedication with medetomidine alone and in combination with MK-467 or glycopyrrolate in dogs subsequently anesthetized with isoflurane.
Bennett, RC; Kuusela, E; Raekallio, MR; Salla, KM; Scheinin, M; Tuns, CI; Vainio, OM, 2017
)
0.94
" Sevoflurane requirement, cardiovascular function, and induction/recovery quality were compared between horses maintained with sevoflurane in combination with medetomidine CRI (3 µg/kg/h) (Group M; n = 25) and those maintained with sevoflurane in combination with alfaxalone-medetomidine CRI (0."( Clinical evaluation of constant rate infusion of alfaxalone-medetomidine combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery.
Ito, H; Kushiro, A; Maeda, T; Nagata, SI; Ohta, M; Okano, A; Tokushige, H; Wakuno, A, 2018
)
0.92
" Sevoflurane in combination with alfaxalone-medetomidine CRI may be a clinically effective anesthetic technique for Thoroughbred racehorses."( Clinical evaluation of constant rate infusion of alfaxalone-medetomidine combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery.
Ito, H; Kushiro, A; Maeda, T; Nagata, SI; Ohta, M; Okano, A; Tokushige, H; Wakuno, A, 2018
)
0.98
"The aim of this study was to investigate the sedative effects of medetomidine in combination with midazolam or butorphanol for routine imaging procedures in dogs."( Randomised clinical trial comparing clinically relevant sedation outcome measures in dogs after intramuscular administration of medetomidine in combination with midazolam or butorphanol for routine diagnostic imaging procedures.
Le Chevallier, D; Murrell, JC; Slingsby, L, 2018
)
0.92
"The aim of the present study was to evaluate clinical efficacy of constant rate infusions (CRIs) of medetomidine-propofol combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery."( Clinical effects of constant rate infusions of medetomidine-propofol combined with sevoflurane anesthesia in Thoroughbred racehorses undergoing arthroscopic surgery.
Arima, D; Ito, H; Kambayashi, Y; Minamijima, Y; Ohta, M; Okano, A; Tokushige, H, 2018
)
0.95
" Administration of midazolam in combination with medetomidine resulted in 71% of dogs displaying paradoxical behaviours (p < 0."( Use of midazolam in combination with medetomidine for premedication in healthy dogs.
Le Chevallier, D; Murrell, J; Slingsby, L, 2019
)
1.04
" This drug combination IV is not recommended for premedication in healthy dogs."( Use of midazolam in combination with medetomidine for premedication in healthy dogs.
Le Chevallier, D; Murrell, J; Slingsby, L, 2019
)
0.79
" The aim of this study was to evaluate in an avian species the influence of isoflurane and sevoflurane on BIS, each at different minimum anaesthetic concentrations (MAC) multiples, alone or combined with butorphanol or medetomidine."( Effects of isoflurane and sevoflurane alone and in combination with butorphanol or medetomidine on the bispectral index in chickens.
Hatt, JM; Martin Jurado, O; Velasco Gallego, ML, 2021
)
1.03
" Each animal was randomly assigned to receive either 80 µg/kg (group L) or 100 µg/kg (group H) medetomidine, combined with 3 mg/kg tiletamine-zolazepam administered intramuscularly."( Comparison of the Cardiovascular Effects of Two Medetomidine Doses Combined with Tiletamine-Zolazepam for the Immobilization of Red Deer Hinds (Cervus elaphus).
Einwaller, J; Habe, M; Painer, J; Pohlin, F; Rauch, H; Stalder, G, 2022
)
1.2
"To evaluate the effects of IM and IV administration of alfaxalone alone and in combination with medetomidine, midazolam, or both on key stress-related neurohormonal and metabolic changes in isoflurane-anesthetized cats undergoing ovariohysterectomy or castration."( A randomized clinical trial on effects of alfaxalone combined with medetomidine and midazolam in preventing stress-related neurohormonal and metabolic responses of isoflurane-anesthetized cats undergoing surgery.
Hikasa, Y; Kamohara, H; Kamohara, T, 2022
)
1.18
"Compared with baseline concentrations, plasma adrenaline and noradrenaline concentrations decreased during anesthesia in cats premedicated with alfaxalone alone and in combination with medetomidine."( A randomized clinical trial on effects of alfaxalone combined with medetomidine and midazolam in preventing stress-related neurohormonal and metabolic responses of isoflurane-anesthetized cats undergoing surgery.
Hikasa, Y; Kamohara, H; Kamohara, T, 2022
)
1.15

Bioavailability

The percentage bioavailability of dexmedetomidine administered intramuscularly compared with the same dose administered intravenously was 73 +/- 11% (mean +/- SD). The bioavailability of dexmedeomidine from the TD preparation was 51%. >100 μg kg(-1)

ExcerptReferenceRelevance
" The bioavailability of dexmedetomidine from the TD preparation was 51%."( Pharmacokinetics and pharmacodynamics of transdermal dexmedetomidine.
Kallio, A; Kivistö, KT; Neuvonen, PJ, 1994
)
0.83
" The percentage bioavailability of dexmedetomidine administered intramuscularly compared with the same dose administered intravenously was 73 +/- 11% (mean +/- SD)."( The pharmacokinetics and hemodynamic effects of intravenous and intramuscular dexmedetomidine hydrochloride in adult human volunteers.
Dyck, JB; Haack, C; Maze, M; Shafer, SL; Vuorilehto, L, 1993
)
0.78
" >100 μg kg(-1)), further investigations into the barriers of medetomidine bioavailability from the sheep gut, liver-bypass drug delivery systems, or other α2-adrenergic agonists (e."( The bioavailability of medetomidine in eight sheep following oesophageal administration.
Hyndman, TH; Maker, GL; Murdoch, FR; Musk, GC; Whittem, T, 2015
)
0.97

Dosage Studied

Medetomidine significantly reduces propofol dosage requirements. Dose-response curve data were obtained with fentanyl, clonidine, xylazine, dexmedetomalid, and 40. At the conclusion of the procedures, three animals were injected with atipamezole IM.

ExcerptRelevanceReference
"5 to 60 degrees C resulted in right shifts in the dose-response curves for all agents with the magnitude of shift being: 1) greatest on the blood pressure and least on the tail flick, and 2) greatest for ST-91 and CLON and least for DMET."( Suppression by spinal alpha-2 agonists of motor and autonomic responses evoked by low- and high-intensity thermal stimuli.
Saeki, S; Yaksh, TL, 1992
)
0.28
" The present results suggest that the dose-response curve of dexmedetomidine for impairment of learning/memory differs between the passive avoidance and water maze tasks."( The effects of dexmedetomidine, an alpha 2 agonist, on learning and memory, assessed using passive avoidance and water maze tasks in rats.
Ekonsalo, T; Lammintausta, R; Riekkinen, P; Riekkinen, PJ; Sirviö, J, 1992
)
0.86
" Rats were administered midazolam, dexmedetomidine, or a combination of midazolam and dexmedetomidine intravenously to derive three dose-response curves for loss of righting reflex (LRR)."( Synergistic interaction between alpha 2-adrenergic agonists and benzodiazepines in rats.
Maze, M; Reid, K; Salonen, M, 1992
)
0.55
" The study was conducted in two parts, the first of which was an open dose-response study that comprised 14 women undergoing abdominal hysterectomy."( Dexmedetomidine infusion for maintenance of anesthesia in patients undergoing abdominal hysterectomy.
Aho, M; Erkola, O; Kallio, A; Korttila, K; Scheinin, H, 1992
)
0.9
" The dose-response curve of medetomidine resembles that of guanfacine, another alpha-2 agonist."( Effects of medetomidine, an alpha-2 adrenoceptor agonist, and atipamezole, an alpha-2 antagonist, on spatial memory performance in adult and aged rats.
Carlson, S; Mecke, E; Pertovaara, A; Rämä, P; Tanila, H, 1992
)
0.97
" Medetomidine at a dosage of 30 micrograms/kg produced more potent sedation than xylazine."( Sedative effects of medetomidine in pigs.
Ishiguro, T; Nishimura, R; Sakaguchi, M; Sasaki, N; Takeuchi, A; Tamura, H, 1992
)
1.52
"1-810 nmol) caused a rightward shift of dose-response curve and reduction of maximal effect of alpha-2 agonists used."( Relative efficacy of spinal alpha-2 agonists, dexmedetomidine, clonidine and ST-91, determined in vivo by using N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible antagonist.
Takano, Y; Yaksh, TL, 1991
)
0.54
" The dose-response curves of medetomidine and its analogs showed that the ranked order of intrinsic activity at lowering IOP was medetomidine greater than or equal to MPV-1440 greater than detomidine greater than MPV-1441 and MPV-305 BII."( Ocular hypotensive effects of medetomidine and its analogs.
Elko, EE; Jin, Y; Wilson, S; Yorio, T, 1991
)
0.86
" The A50 (dose producing 50% MPE) for each drug or drug combination was determined from the dose-response curve."( Antinociceptive interaction between opioids and medetomidine: systemic additivity and spinal synergy.
Bagley, J; Harris, S; Lin, BS; Lloyd, P; Messineo, E; Ossipov, MH, 1990
)
0.53
" According to the laboratorical determinations, regardless of the dosage and the route of application, medetomidine did not affect the AST and AP enzyme activities, or the BUN and creatinine values."( Clinical investigations of medetomidine in dogs.
Mora, S; Romváry, A; Simon, F, 1989
)
0.79
" When the dosage was 40 micrograms/kg (22 dogs), treatment was successful in 55% of cases respectively."( Suturation of wounds of extremities in dogs using medetomidine as sedative and analgesic drug.
Sarkiala, E, 1989
)
0.53
" Differences between dosing routes were small."( Pharmacokinetics of medetomidine.
Salonen, JS, 1989
)
0.6
" Neostigmine was injected either 20 or 60 minutes prior to beginning cumulative dosing with the alpha 2-adrenergic agonist."( Subarachnoid neostigmine potentiation of alpha 2-adrenergic agonist analgesia. Dexmedetomidine versus Clonidine.
Bouaziz, H; Eisenach, JC; Hewitt, C,
)
0.36
" Glycopyrrolate was administered IV and IM at a dosage of 11 micrograms/kg of body weight, each."( Alterations in the arrhythmogenic dose of epinephrine after xylazine or medetomidine administration in halothane-anesthetized dogs.
Benson, GJ; Lemke, KA; Olson, WA; Thurmon, JC; Tranquilli, WJ, 1993
)
0.52
" Glycopyrrolate was administered IV and IM at a dosage of 11 micrograms/kg of body weight, each."( Alterations in the arrhythmogenic dose of epinephrine after xylazine or medetomidine administration in isoflurane-anesthetized dogs.
Benson, GJ; Lemke, KA; Olson, WA; Thurmon, JC; Tranquilli, WJ, 1993
)
0.52
" Mydriasis appeared on administration of a 1 microgram dose and its degree was proportional to the dexmedetomidine dosage up to 12 micrograms."( Mydriatic and antinociceptive effects of intrathecal dexmedetomidine in conscious rats.
Benedek, G; Horváth, G; Kovács, M; Szikszay, M, 1994
)
0.75
" The combination of an opioid with DMED might reduce the dosage requirements for each drug and thereby allow the same anesthetic depth to be achieved with lesser degrees of their individual side effects."( Anesthetic and hemodynamic interactions of dexmedetomidine and fentanyl in dogs.
Hug, CC; Salmenperä, MT; Szlam, F, 1994
)
0.55
" dose-response curves were obtained with dexmedetomidine, clonidine and ST-91 in groups of rats which had received a 7-day infusion of saline or the equianalgesic concentrations of dexmedetomidine (10 nmol/hr) or ST-91 (30 nmol/hr)."( Chronic spinal infusion of dexmedetomidine, ST-91 and clonidine: spinal alpha 2 adrenoceptor subtypes and intrinsic activity.
Takano, Y; Yaksh, TL, 1993
)
0.84
" Microinjections of medetomidine into the cerebellum or the PAG produced an identical dose-response curve in the tail-flick test as that obtained following microinjection into the RVM."( The rostroventromedial medulla is not involved in alpha 2-adrenoceptor-mediated antinociception in the rat.
Hämäläinen, MM; Pertovaara, A, 1993
)
0.61
" Medetomidine significantly reduces propofol dosage requirements."( Comparative responses to propofol anaesthesia alone and with alpha 2-adrenergic medications in a canine model.
Bufalari, A; Giannoni, C; Short, CE; Vainio, O, 1996
)
1.2
" The decrease in 5-HT turnover more closely correlated with the dose-response curve for loss of righting reflex, a behavioral measure of hypnosis, than did the norepinephrine turnover."( Role of serotonergic neurotransmission in the hypnotic response to dexmedetomidine, an alpha 2-adrenoceptor agonist.
Gregg, K; Guo, TZ; Maze, M; Rabin, BC, 1996
)
0.53
"kg-1), doses in the steep part of the dose-response curve."( Sympatholytic and minimum anesthetic concentration-sparing responses are preserved in rats rendered tolerant to the hypnotic and analgesic action of dexmedetomidine, a selective alpha(2)-adrenergic agonist.
Guo, TZ; Gustafsson, E; Maze, M; Rabin, BC; Reid, K; Zhang, C, 1996
)
0.49
" Dose-response analyses showed that dexmedetomidine, epinephrine, norepinephrine had similar analgesic potencies, but clonidine was significantly less potent."( Spinal administration of adrenergic agents produces analgesia in amphibians.
Brenner, GM; Stevens, CW, 1996
)
0.56
" Dose-response curve data were obtained with fentanyl, clonidine, xylazine, dexmedetomidine, and 40."( Alpha 2-adrenoceptor agonists and stress-induced analgesia in rats: influence of stressors and methods of analysis.
De Kock, M; Meert, TF, 1997
)
0.52
" Oral dosing of diazinon at 75 and 100 mg/kg produced signs of toxicosis in mice characteristic of cholinergic over-stimulation, and the percentages of deaths were 90 and 100%, respectively."( Medetomidine protection against diazinon-induced toxicosis in mice.
Mohammad, FK; Yakoub, LK, 1997
)
1.74
"The low dosage of medetomidine (0."( Cardiovascular effects of the alpha2-adrenergic receptor agonist medetomidine in clinically normal cats anesthetized with isoflurane.
Bright, JM; Daniel, GB; Fefee, D; Golden, AL; Harvey, RC; Schmidt, D, 1998
)
0.87
" Medetomidine was administered intramuscularly at a dose of 1000 micrograms/m2 body surface area 10 to 15 minutes before the induction of anaesthesia by the administration of propofol (n = 44) or ketamine (n = 40) dosed to effect."( Clinical efficacy and safety of propofol or ketamine anaesthesia in dogs premedicated with medetomidine.
Hellebrekers, LJ; Hird, JF; Rosenhagen, CU; Sap, R; Vainio, O; van Herpen, H, 1998
)
1.43
" Yohimbine pretreatment resulted in a rightward shift of the dose-response curves (DMET > CLON > UK)."( Pharmacological evidence for different alpha 2-adrenergic receptor sites mediating analgesia and sedation in the rat.
Buerkle, H; Yaksh, TL, 1998
)
0.3
" When using IV medetomidine, a reduction of the recommended dosage (ie, +/-30 to 40 microg/kg) by up to 6 times did not significantly influence the cardiovascular effects."( Hemodynamic effects of medetomidine in the dog: a dose titration study.
Pypendop, BH; Verstegen, JP,
)
0.79
" Dose-response data show dexmedetomidine to be the most potent inhibitor."( Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds.
Hébert, CA; Kudo, LH; Rouch, AJ, 1999
)
0.6
"To develop a dosage correlated with shoulder height (SH) in centimeters for effective immobilization of free-ranging giraffes, using a combination of medetomidine (MED) and ketamine (KET) and reversal with atipamezole (ATP)."( Use of medetomidine and ketamine for immobilization of free-ranging giraffes.
Bush, M; Grobler, DG; Lance, WR; Phillips, LG; Raath, JP; Stamper, MA, 2001
)
0.96
" The iteration and the prediction procedures may be used to reduce the number of experimental animals in dose-response studies in other species."( Determination of optimal immobilizing doses of a medetomidine hydrochloride and ketamine hydrochloride combination in captive reindeer.
Arnemo, JM; Larsen, S; Ryeng, KA, 2001
)
0.57
" Thirty healthy adult turtles were assigned randomly to one of two dosage groups."( Medetomidine-ketamine anesthesia in red-eared slider turtles (Trachemys scripta elegans).
Diggs, HE; Greer, LL; Jenne, KJ, 2001
)
1.75
" A dose-response effect was observed in all groups except for the Med-160 group."( Effect of medetomidine on electroencephalography and use of a quantitative electroencephalograph for evaluating sedation levels in dogs.
Itamoto, K; Matsumura, H; Miyara, T; Taga, A; Takuma, T; Taura, Y; Wada, N, 2001
)
0.71
" By reducing the dosage of Medetomidine, reduced cardio-respiratory side-effects are to be expected."( [Medetomidine-butorphanol combination anesthesia in the dog].
Boschung, H; Busato, A; Güller, K; Lang, MJ, 2001
)
1.52
" Anesthesia was rapidly and completely reversed by intravenous injections of naltrexone at 30 times the THAI dosage (0."( Anesthesia of boma-captured Lichtenstein's hartebeest (Sigmoceros lichtensteinii) with a combination of thiafentanil, medetomidine, and ketamine.
Bush, M; Citino, SB; Grobler, D; Lance, W, 2002
)
0.52
" An initial dose-response trial determined the efficacy of either propofol (3."( Evaluation of propofol and medetomidine-ketamine for short-term immobilization of Gulf of Mexico sturgeon (Acipenser oxyrinchus de soti).
Fleming, GJ; Francis Floyd, R; Heard, DJ; Riggs, A, 2003
)
0.62
"This study was performed to determine the optimal reversal dosage of atipamezole on medetomidine-ketamine combination anesthesia."( Reversal of medetomidine-ketamine combination anesthesia in rabbits by atipamezole.
Jeong, SM; Kim, MS; Nam, TC; Park, JH; Seo, KM, 2004
)
0.93
") 10 min after anesthetic induction, and group 2 received the same dosage at 20 min post-induction."( Tribromoethanol-medetomidine combination provides a safe and reversible anesthetic effect in Sprague-Dawley rats.
Bay, TN; Brown, SR; Gopalan, C; Hegade, GM; Talcott, MR, 2005
)
0.67
" The optimum dosage for nyala was a combination of A3080 (40-50 microg/kg), MED (60-80 microg/kg) plus 200 mg of KET/animal."( Anaesthesia of nyala (Tragelaphus angasi) with a combination of thiafentanil (A3080), medetomidine and ketamine.
Bush, M; Cooper, DV; Grobler, D; Jessup, D; Lance, W, 2005
)
0.55
" Dosage C in contrast had fewer side effects but less favourable cardiovascular results and a longer recovery period."( A comparative clinical study of three different dosages of intramuscular midazolam-medetomidine-ketamine immobilization in cats.
Busch, R; Ebner, J; Erhardt, W; Henke, J; Wehr, U, 2007
)
0.56
" The addition of flumazenil showed no significant difference to atipamezole alone, but subcutaneous administration of atipamezole alone was not sufficient in the dosage used to show an advantage compared to non-reversed cats."( Partial antagonization of midazolam-medetomidine-ketamine in cats--atipamezole versus combined atipamezole and flumazenil.
Baumgartner, C; Ebner, J; Erhardt, W; Henke, J; Wehr, U, 2007
)
0.61
" In addition, the effects of dosing route on haematological stress markers were evaluated."( The efficacy of orally dosed ketamine and ketamine/medetomidine compared with intramuscular ketamine in rhesus macaques (Macaca mulatta) and the effects of dosing route on haematological stress markers.
Bates, WA; Feng, C; Winterborn, AN; Wyatt, JD, 2008
)
0.6
" Animals were trained to accept oral dosing and then randomly assigned to one of three drug regimens: (1) ketamine IM, (2) ketamine PO, (3) Ketamine/medetomidine PO."( The efficacy of orally dosed ketamine and ketamine/medetomidine compared with intramuscular ketamine in rhesus macaques (Macaca mulatta) and the effects of dosing route on haematological stress markers.
Bates, WA; Feng, C; Winterborn, AN; Wyatt, JD, 2008
)
0.8
"Oral dosing alone was not sufficient to achieve a plane of sedation that allowed for safe handling."( The efficacy of orally dosed ketamine and ketamine/medetomidine compared with intramuscular ketamine in rhesus macaques (Macaca mulatta) and the effects of dosing route on haematological stress markers.
Bates, WA; Feng, C; Winterborn, AN; Wyatt, JD, 2008
)
0.6
" Leukogram profiles indicated that orally dosed animals experienced a higher level of stress."( The efficacy of orally dosed ketamine and ketamine/medetomidine compared with intramuscular ketamine in rhesus macaques (Macaca mulatta) and the effects of dosing route on haematological stress markers.
Bates, WA; Feng, C; Winterborn, AN; Wyatt, JD, 2008
)
0.6
" Complete immobilization and excellent induction quality was achieved with a low volume dosage of BAM-2."( Butorphanol-azaperone-medetomidine for immobilization of captive white-tailed deer.
Howze, MB; Lance, WR; Miller, BF; Miller, KV; Osborn, DA; Warren, RJ, 2009
)
0.67
" Recently, data suggested that following intravenous infusion at six dosing regiments non-linear pharmacokinetics was observed."( Metabolic stability and determination of cytochrome P450 isoenzymes' contribution to the metabolism of medetomidine in dog liver microsomes.
Beaudry, F; Duhamel, MC; Troncy, E, 2010
)
0.58
" On the basis of rapid, smooth, and successful inductions and recoveries, the described dosage of thiafentanil and medetomidine, with administration of midazolam prior to recovery, is recommended for immobilization of adult emus."( Use of thiafentanil-medetomidine for the induction of anesthesia in emus (Dromaius novaehollandiae) within a wild animal park.
Cushing, A; McClean, M, 2010
)
0.89
" At the conclusion of the procedures, 70 min after medetomidine administration, three animals were injected with atipamezole IM into the opposite triceps muscle at a dosage based on body surface area."( Medetomidine immobilisation and atipamezole reversal in large estuarine crocodiles (Crocodylus porosus) using metabolically scaled dosages.
Olsson, A; Phalen, D, 2012
)
2.07
"Medetomidine at a metabolically scaled dosage delivered IM into the forelimb was effective for immobilising large estuarine crocodiles for at least 40 min."( Medetomidine immobilisation and atipamezole reversal in large estuarine crocodiles (Crocodylus porosus) using metabolically scaled dosages.
Olsson, A; Phalen, D, 2012
)
3.26
" The total Telazol dosage was also significantly different between young lemurs (33 +/- 15 mg/kg) and mature lemurs (18 +/- 9 mg/kg)."( Field anesthesia of wild ring-tailed lemurs (Lemur catta) using tiletamine-zolazepam, medetomidine, and butorphanol.
Cuozzo, FP; Larsen, RS; Moresco, A; Sauther, ML, 2011
)
0.59
" Notably, an unacceptable long recovery period in both ketamine/medetomidine protocols (subsequently reversed with atipamezole) was observed, showing that α-2 adrenoreceptor agonists in the used dose and dosing regime is not the first choice for sedation in common marmosets in a standard research setting."( Comparison of three different sedative-anaesthetic protocols (ketamine, ketamine-medetomidine and alphaxalone) in common marmosets (Callithrix jacchus).
Bakker, J; Brok, HP; Langermans, JA; Pelt, ER; Remarque, EJ; Uilenreef, JJ, 2013
)
0.85
" However, the higher dosage needed compared to rats may suppress the functional synchrony and lead to unilateral connectivity."( Detection of functional connectivity in the resting mouse brain.
Chuang, KH; Nasrallah, FA; Tay, HC, 2014
)
0.4
" Secondly, we examined how different dosage and optimum injection timing of ATI affected mice recovery from anesthesia."( Anesthetic effects of a three-drugs mixture--comparison of administrative routes and antagonistic effects of atipamezole in mice.
Kirihara, Y; Kobayashi, Y; Kurosaki, K; Saito, Y; Takechi, M; Takeuchi, T, 2015
)
0.42
" The dosage and drug combination used was effective for immobilization of ABBs with minimal adverse effects on vital signs and can be recommended in most clinical applications."( Immobilization of Asiatic Black Bears ( Ursus thibetanus ) with Medetomidine-Zolazepam-Tiletamine in South Korea.
Jeong, DH; Seok, SH; Song, BC; Yang, JJ; Yeon, SC, 2017
)
0.69
" During anaesthesia, minor veterinary procedures such a blood collection, intubation, vaccination and collaring could safely be performed with no additional dosing required."( Evaluation of BAM (butorphanol-azaperone-medetomidine) in captive African lion (Panthera leo) immobilization.
Andrianov, V; Laubscher, L; Orro, T; Pfitzer, S; Raath, JP; Semjonov, A; Venter, D, 2017
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)3.40000.00001.44217.3470AID35925
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki1.11000.00010.949010.0000AID37293
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.02500.00000.929610.0000AID37072; AID37076
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.02500.00000.970810.0000AID37072; AID37076
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.02500.00000.937510.0000AID37072; AID37076
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki1.11000.00000.575110.0000AID37293
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki1.11000.00000.965010.0000AID37293
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)0.28100.00132.612925.7000AID36578
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)0.28100.00133.394625.7000AID36578
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)0.28100.00133.394625.7000AID36578
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID37173Alpha-1 adrenergic receptor binding affinity in rat brain membranes1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID37293Displacement of [3H]-prazosin from Alpha-1 adrenergic receptor of rat brain membranes1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".
AID37393Tested for its binding affinity against alpha-2 receptor in rat brain membrane1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID35423Tested for its binding affinity against alpha-1 receptor in rat brain membrane1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID35925Tested for its ability to antagonize epinephrine induced primary wave aggregation in human platelets at alpha-2A-adrenergic receptor sites.1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID3657850% Molar effective concentration afainst Alpha-1 adrenergic receptor in rat aorta1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID37076Displacement of [3H]rauwolscine from Alpha-2 adrenergic receptor of rat brain membranes1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".
AID233034Relative affinity for Alpha 2 over Alpha 1 adrenergic receptors1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".
AID232985Ratio between IC50 values of alpha 1 and alpha 2 receptors1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID37072Alpha-2 adrenergic receptor binding affinity was tested against membrane preparations of rat brain.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID229907Selectivity ratio of Ki of alpha-1 adrenergic receptor to alpha-2 receptor1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID232984Ratio between EC50 values of alpha 1 and alpha 2 receptors1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID36585Percent maximal response to Alpha-1 adrenergic receptor in rat aorta which is relative to phenylephrine1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID35987Tested for its inhibitory activity against alpha-1 adrenoceptor in guinea pig ileum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID36183Alpha-2 adrenergic receptor antagonistic activity in human blood platelets.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
AID36046Tested for its inhibitory activity against alpha-2 adrenoceptor in guinea pig ileum1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
AID226738Alpha 2 antagonistic adrenoceptor activity in human blood platelets Potency ratio: IC50(medetomidine)/IC50(analog)1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,295)

TimeframeStudies, This Drug (%)All Drugs %
pre-199053 (4.09)18.7374
1990's474 (36.60)18.2507
2000's282 (21.78)29.6817
2010's379 (29.27)24.3611
2020's107 (8.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 63.45

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index63.45 (24.57)
Research Supply Index7.40 (2.92)
Research Growth Index5.43 (4.65)
Search Engine Demand Index109.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (63.45)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials296 (22.17%)5.53%
Reviews19 (1.42%)6.00%
Case Studies18 (1.35%)4.05%
Observational0 (0.00%)0.25%
Other1,002 (75.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]