Page last updated: 2024-11-04

xylazine

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Description

Xylazine: An adrenergic alpha-2 agonist used as a sedative, analgesic and centrally acting muscle relaxant in VETERINARY MEDICINE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

xylazine : A methyl benzene that is 1,3-dimethylbenzene which is substituted by a 5,6-dihydro-4H-1,3-thiazin-2-ylnitrilo group at position 2. It is an alpha2 adrenergic receptor agonist and frequently used in veterinary medicine as an emetic and sedative with analgesic and muscle relaxant properties. [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]

Cross-References

ID SourceID
PubMed CID5707
CHEMBL ID297362
CHEBI ID92386
SCHEMBL ID15487
MeSH IDM0023071

Synonyms (162)

Synonym
AB00052246-15
AB00052246-16
BRD-K21565985-001-05-0
bayer 1470
gtpl523
KBIO1_000449
DIVK1C_000449
smr000061135
MLS000054617 ,
SPECTRUM_001267
LOPAC0_001249
PRESTWICK_962
xylazine
7361-61-7
NCGC00016098-02
cas-7361-61-7
lopac-x-1251
NCGC00016098-01
BCBCMAP01_000167
PRESTWICK2_000598
BSPBIO_000476
PRESTWICK3_000598
IDI1_000449
BPBIO1_000524
SMP1_000319
BSPBIO_003023
SPECTRUM5_001250
xylazine, >=99%
NCGC00038586-02
NCGC00038586-03
NCGC00038586-05
2-(2,6-dimethylphenylamino)-4h-5,6-dihydro-1,3-thiazine
5,6-dihydro-2-(2,6-xylidino)-4h-1,3-thiazine
4h-1,3-thiazin-2-amine, n-(2,6-dimethylphenyl)-5,6-dihydro-
bay 1470
2-(2,6-dimethylanilino)-5,6-dihydro-4h-1,3-thiazine
xylazinum [inn-latin]
4h-1,3-thiazine, 5,6-dihydro-2-(2,6-xylidino)-
2,6-xylidine, n-(5,6-dihydro-4h-1,3-thiazinyl)-
einecs 230-902-1
wh 7286
xilazina [inn-spanish]
4h-1,3-thiazine-2-amine, n-(2,6-dimethylphenyl)-5,6-dihydro-
xylazin
xylaxine
n-(2,6-dimethylphenyl)-5,6-dihydro-4h-1,3-thiazin-2-amine
KBIO3_002523
KBIOSS_001747
KBIO2_004315
KBIO2_006883
KBIOGR_000937
KBIO2_001747
PRESTWICK0_000598
SPECTRUM3_001472
SPBIO_002695
SPECTRUM2_001448
NINDS_000449
PRESTWICK1_000598
SPECTRUM4_000239
SPBIO_001315
SPECTRUM1501200
NCGC00038586-04
MLS000881122
HMS2092L07
HMS2089E20
NCGC00016098-08
nsc-758142
CHEMBL297362 ,
chanazine
AKOS000115960
L001033
D08683
chanazine (tn)
xylazine (usp/inn)
HMS501G11
FT-0654963
HMS1921P17
HMS1569H18
rometar
(5,6-dihydro-4h-[1,3]thiazin-2-yl)-(2,6-dimethyl-phenyl)-amine
bdbm50027069
(2,6-dimethyl-phenyl)-[1,3]thiazinan-2-ylidene-amine
NCGC00016098-07
A837877
HMS2096H18
nsc758142
pharmakon1600-01501200
dtxsid3040643 ,
dtxcid1020643
tox21_110303
HMS2232F24
CCG-39193
NCGC00016098-04
NCGC00016098-09
NCGC00016098-06
NCGC00016098-03
NCGC00016098-05
nsc 758142
primazine
sedomin
xilazina
unii-2kfg9tp5v8
xylazinum
xylazine [usp:inn:ban]
2kfg9tp5v8 ,
xylazine(rompun)
BCP0726000235
xylazine-d6
xylazine [green book]
xylazine [inn]
xylazine [usp-rs]
xylazine [mi]
tranq component xylazine
xylazine [mart.]
xylazine [usp monograph]
S10383
S5564
HMS3369L20
HY-B0443
AB00052246-13
SCHEMBL15487
tox21_110303_1
NCGC00016098-11
xylapan (salt/mix)
xylasol (salt/mix)
narcoxyl
xylzin
rompun (salt/mix)
AC-22589
xylazine free base
OPERA_ID_1260
AB00052246_18
AB00052246_17
mfcd00057908
sr-01000075296
xilazine
CHEBI:92386 ,
n-(5,6-dihydro-4h-1,3-thiazinyl)-2,6-xylidine
SR-01000075296-4
SR-01000075296-6
SBI-0051216.P003
(5,6-dihydro-4h-[1,3]thiazin-2-yl)-(2,6-dimethyl-phenyl)-amine;n-(2,6-dimethylphenyl)-5,6-dihydro-4h-1,3-thiazin-2-amine
xylazine (free base)
HMS3713H18
AS-54468
Q426081
SY110316
Z56828371
DB11477
BCP03045
bdbm50225286
BRD-K21565985-001-15-9
EN300-02865
SDCCGSBI-0051216.P004
HMS3886E12
NCGC00016098-23
xilazina (inn-spanish)
xylazinum (inn-latin)
xylazine (usp monograph)
xylazine (mart.)
xylazine (usp-rs)
xylazine (usp:inn:ban)

Research Excerpts

Overview

Xylazine is a veterinary tranquilizer, long noted in the street opioid supply of Puerto Rico, and more recently Philadelphia. It is an alpha-2 receptor agonist that is not approved for human use but is commonly used in veterinary medicine due to its sedative and muscle-relaxant properties.

ExcerptReferenceRelevance
"Xylazine is an alpha-2 adrenergic agonist commonly used as a large animal anesthetic. "( Management of Xylazine Withdrawal in a Hospitalized Patient: A Case Report.
Ehrman-Dupre, R; Haroz, R; Kaigh, C; Peterson, LK; Salzman, M; Schmidt, R,
)
1.93
"Xylazine is a veterinary tranquilizer, long noted in the street opioid supply of Puerto Rico, and more recently Philadelphia."( Xylazine spreads across the US: A growing component of the increasingly synthetic and polysubstance overdose crisis.
Bourgois, P; Dye, D; Friedman, J; Goodman-Meza, D; Montero, F; Shover, C; Wahbi, R, 2022
)
2.89
"Xylazine is an alpha-2-adrenergic agonist used for its sedative and analgesic properties in veterinary medicine. "( Xylazine poisoning: a systematic review.
Ball, NS; Covvey, JR; Gionfriddo, MR; Guarascio, AJ; Knable, BM; Montepara, CA; Nemecek, BD; Relich, TA; Smathers, AN; Zimmerman, DE, 2022
)
3.61
"Xylazine is a tranquilizer commonly added into the illicit drug supply and a likely contributor to overdoses because it does not respond to naloxone reversal. "( Widespread Distribution of Xylazine Detected Throughout the United States in Healthcare Patient Samples.
Heltsley, R; Holt, AC; Le, K; Schrecker, JP; Schwope, DM,
)
1.87
"Xylazine is an alpha-2 receptor agonist that is not approved for human use but is commonly used in veterinary medicine due to its sedative and muscle-relaxant properties."( Pharmacology and toxicology of xylazine: quid novum?
Berretta, P; Busardò, FP; Kapoor, A; Malaca, S; Pesaresi, M; Pirani, F, 2023
)
1.92
"Xylazine is an animal sedative, approved by the U.S. "( Xylazine Adulteration of the Heroin-Fentanyl Drug Supply : A Narrative Review.
D'Orazio, J; Haroz, R; Nelson, L; Perrone, J; Wightman, R, 2023
)
3.8
"Xylazine is an α 2 -agonist increasingly prevalent in the illicit drug supply. "( Self-reported Xylazine Experiences: A Mixed-methods Study of Reddit Subscribers.
Lakamana, S; Love, JS; O'Connor, K; Perrone, J; Sarker, A; Spadaro, A; Wightman, R,
)
1.93
"Xylazine is an α 2 -adrenergic agonist that is commonly used as a veterinary tranquilizer and is increasingly present in the unregulated US drug supply since at least 2019. "( Recognition and Treatment of Wounds in Persons Using Xylazine: A Case Report From New Haven, Connecticut.
Barelli, P; Doernberg, M; Dowton, A; Golden, M; Heiman, E; Leventhal, J; Morford, KL; Sue, KL; Wang, H,
)
1.82
"Xylazine is an unscheduled non-opioid indicated as a veterinary tranquilizer, also known as "Tranq." This drug is commonly used in combination with other drugs, such as heroin, fentanyl, and cocaine."( Xylazine: The Drug Taking the World By Storm: What You Need to Know.
Brown, W; Mumba, MN; Tice, J, 2023
)
3.07
"Xylazine is an α"( α
Di Marzo, V; Duarte, IDG; Miranda E Castor, MG; Parrella, C; Piscitelli, F; Romero, TRL, 2020
)
2
"Xylazine is an emerging adulterant with fentanyl in fatal drug intoxications, which has public health, safety, and criminal investigative implications. "( Xylazine, a Veterinary Tranquilizer, Detected in 42 Accidental Fentanyl Intoxication Deaths.
DeJoseph, ME; Gill, JR; Nunez, J, 2021
)
3.51
"Xylazine is an α-2 adrenoreceptor agonist used as a sedative/analgesic in veterinary medicine. "( High prevalence of xylazine among fentanyl screen-positive urines from hospitalized patients, Philadelphia, 2021.
Haviland, KL; Korn, WR; Stickle, DF; Stone, MD; Toohey, JM, 2021
)
2.39
"Xylazine is an α2 -adrenoceptor agonist and it is widely used in veterinary anesthesia in combination with ketamine. "( Characterization of xylazine metabolism in rat liver microsomes using liquid chromatography-hybrid triple quadrupole-linear ion trap-mass spectrometry.
Beaudry, F; Lavoie, DS; Pailleux, F; Vachon, P, 2013
)
2.16
"Xylazine is a potent α2-adrenergic agonist used in veterinary medicine for sedation, analgesia, muscle relaxation, and so on. "( Determination of xylazine and 2,6-xylidine in animal tissues by liquid chromatography-tandem mass spectrometry.
Chen, G; Li, S; Mi, X; Zheng, X, 2013
)
2.17
"Xylazine is a potent analgesic extensively used in veterinary and animal experimentation. "( Xylazine Activates Adenosine Monophosphate-Activated Protein Kinase Pathway in the Central Nervous System of Rats.
Chen, H; Fan, HG; Li, X; Shi, XX; Su, LX; Wang, HB; Yang, P; Yin, BS, 2016
)
3.32
"Xylazine is a sedative, analgesic, anesthetic, and central muscle relaxant approved for animals but not humans. "( Xylazine Exposures Reported to Texas Poison Centers.
Forrester, MB, 2016
)
3.32
"Xylazine is an alpha(2)-adrenoceptor agonist extensively used in veterinary and animal experimentation. "( Probable involvement of alpha(2C)-adrenoceptor subtype and endogenous opioid peptides in the peripheral antinociceptive effect induced by xylazine.
de Castro Perez, A; de Francischi, JN; Gama Duarte, ID; Romero, TR, 2009
)
2
"Xylazine is an alpha(2)-adrenergic agonist extensively used in veterinary medicine and animal experimentation for producing antinociception, sedation, and muscle relaxation. "( Involvement of ATP-sensitive K(+) channels in the peripheral antinociceptive effect induced by the alpha(2)-adrenoceptor agonist xylazine.
Duarte, ID; Romero, TR, 2009
)
2
"Xylazine is a pre-synaptic alpha2-adrenoreceptor agonist which blocks noradrenaline release from the sympathetic system."( Similar half-octave TTS protection of the cochlea by xylazine/ketamine or sympathectomy.
Cazals, Y; Giraudet, F; Horner, KC, 2002
)
1.29
"Xylazine is an alpha2-adrenoceptor agonist sedative with a much higher interspecies variability in effect than detomidine, another alpha2-agonist used in veterinary practice. "( Interactions of xylazine and detomidine with alpha2-adrenoceptors in brain tissue from cattle, swine and rats.
Bergström, U; Neil, A; Törneke, K, 2003
)
2.11
"Xylazine and ketamine are an anesthetic combination used in feline practice for routine surgical procedures. "( Effect of yohimbine on xylazine-ketamine anesthesia in cats.
Hsu, WH; Lu, ZX, 1984
)
2.02
"Xylazine is an effective sedative analgesic that induces vomiting in the cat. "( Emetic action of xylazine on the chemoreceptor trigger zone for vomiting in cats.
Borison, HL; Colby, ED; McCarthy, LE, 1981
)
2.05
"Xylazine is a veterinary sedative, analgesic or general anesthetic. "( Xylazine toxicity--literature review and report of two cases.
Hearn, WL; Hime, GW; Mittleman, RE, 1998
)
3.19
"Xylazine is an effective drug for immobilization of mountain goats captured in traps, at dosages of about 4.9 mg/kg."( Immobilization of mountain goats with xylazine and reversal with idazoxan.
Côté, SD; Festa-Bianchet, M; Haviernick, M, 1998
)
1.29
"Xylazine is an adrenergic alpha(2) agonist, which is used in veterinary medicine as a sedative and anesthetic agent. "( Immunomodulatory effect of xylazine, an alpha(2) adrenergic agonist, on rat spleen cells in culture.
Colić, M; Cupić, V; Pavicić, L; Varagić, VM; Vucević, D, 2001
)
2.05
"Xylazine is a tranquilizer that is widely used in both biomedical research and veterinary medicine. "( Rapid inibition of basal and glucose-stimulated insulin release by xylazine.
Arieff, AI; Goldfine, ID, 1979
)
1.94
"Xylazine was found to be a safe and reliable drug for chemical restraint of Bactrian camels (Camelus bactrianus). "( Hematologic effects of xylazine when used for restraint of Bactrian camels.
Bush, M; Custer, R; Kennedy, S; Kramer, L, 1977
)
2.01
"That xylazine is a partial agonist was verified by the fact that when present in excess, it could stimulate insulin release which had already been inhibited to 100% by epinephrine."( Inhibition of glucose-induced insulin release by xylazine.
Abdel el Motal, SM; Sharp, GW, 1985
)
0.98
"Xylazine is an agent frequently used in combination with ketamine to anesthetize rabbits. "( The ocular effects of xylazine in rabbits, cats, and monkeys.
Burke, JA; Potter, DE, 1986
)
2.03

Effects

Xylazine has emerged in recent years as an adulterant in an increasing number of opioid-positive overdose deaths in the United States. Xylazine alone has proven harmful to humans and even more when it is combined with drugs of abuse.

ExcerptReferenceRelevance
"Xylazine has a strong hyperglycaemic effect due to its blocking of the pancreatic insulin release via stimulation of parasympathetic (alpha 2-adrenergic) receptors. "( Increased glucose content in the aqueous humour caused by the use of xylazine.
Arnbjerg, J; Eriksen, T, 1990
)
1.96
"Xylazine has emerged in recent years as an adulterant in an increasing number of opioid-positive overdose deaths in the United States. "( Xylazine effects on opioid-induced brain hypoxia.
Choi, S; Irwin, MR; Kiyatkin, EA, 2023
)
3.8
"Xylazine has emerged as a consistent part of the unregulated drug supply in recent months. "( Reducing the harms of xylazine: clinical approaches, research deficits, and public health context.
Aronowitz, S; Dasgupta, N; Ferguson, A; Figgatt, M; Hill, LG; Hosey, RA; McElligott, Z; Moraff, C; Stahl, NE; Zagorski, CM, 2023
)
2.67
"Xylazine has taken the world by storm and proactive strategies are urgently needed to combat its negative impacts on population health. "( Xylazine: The Drug Taking the World By Storm: What You Need to Know.
Brown, W; Mumba, MN; Tice, J, 2023
)
3.8
"Xylazine alone has proven harmful to humans and even more when it is combined with drugs of abuse."( Xylazine intoxication in humans and its importance as an emerging adulterant in abused drugs: A comprehensive review of the literature.
Chavez-Arias, C; Díaz-Alcalá, JE; Martínez, MA; Ruiz-Colón, K, 2014
)
2.57
"Xylazine (rompun) has sedative, analgetic and myorelaxative effects; in addition to this, it also influences the homeostasis of glucose in the organism. "( [Changes in blood sugar after administration of xylazine and adrenergic blockers in the rat].
Jasenovec, A; Koppel, J; Kuchár, S; Mozes, S; Petrusová, K, 1982
)
1.96
"Xylazine has been characterized as a selective alpha 2-adrenoceptor agonist, which has explained its central nervous system depressant and other pharmacological effects. "( Probable post-synaptic alpha 2 adrenergic mediated effect of xylazine on goat uterine motility.
Arrue, R; Cox, JF; Perez, R, 1994
)
1.97
"Xylazine has a strong hyperglycaemic effect due to its blocking of the pancreatic insulin release via stimulation of parasympathetic (alpha 2-adrenergic) receptors. "( Increased glucose content in the aqueous humour caused by the use of xylazine.
Arnbjerg, J; Eriksen, T, 1990
)
1.96
"Xylazine has structural similarity to the phenothiazines and pharmacological activity similar to clonidine."( Human overdose with the veterinary tranquilizer xylazine.
Grimes, MJ; Hall, AH; Honea, BN; Rumack, BH; Spoerke, DG, 1986
)
1.25

Actions

Xylazine can cause slight hematologic changes, but without splenic changes. Xylazine is known to cause hyperglycaemia by increasing hepatic glucose production.

ExcerptReferenceRelevance
"Xylazine was used to enhance sedation and ketamine was subsequently administered for induction."( Accelerated Idioventricular Rhythm Associated With Isoflurane Administration in a Foal: A Case Report.
Manso-Díaz, G; Peña-Cadahia, C; Santiago-Llorente, I; Villalba-Orero, M, 2019
)
1.24
"Xylazine can cause slight hematologic changes, but without splenic changes."( Hematological and splenic Doppler ultrasonographic changes in dogs sedated with acepromazine or xylazine.
Antunes, RR; Beier, SL; Comassetto, F; Costa, Á; Mattoso, CRS; Muller, TR; Saito, ME; Sutil, DV; Tochetto, R; Volpato, J; Weinert, NC, 2017
)
1.39
"Xylazine is known to cause hyperglycaemia by increasing hepatic glucose production. "( Effect of xylazine on plasma glucose, glucagon and insulin concentrations in sheep.
Brockman, RP, 1981
)
2.11

Treatment

Treatment with xylazine was associated with an overall increased FSH and LH pulse frequency, compared with that observed during 12-h pretreatment periods. Xylazine pretreatment also protected rats against electroshock-induced convulsions.

ExcerptReferenceRelevance
"Xylazine-treated groups had higher cortisol than saline-treated animals and showed no differences among them at any time."( Effect of hot-iron disbudding on behaviour and plasma cortisol of calves sedated with xylazine.
Broom, DM; Carolino, N; Carvalho, RC; Lima, MS; Stilwell, G, 2010
)
1.31
"All xylazine-treated cows showed signs of mild sedation, a reduced pain response on insertion of the needle for LA, reduced ear flicking during surgery, reduced lameness score and longer standing periods as well as improved appetite in the first hour postoperatively."( The use of xylazine hydrochloride in an analgesic protocol for claw treatment of lame dairy cows in lateral recumbency on a surgical tipping table.
Herdtweck, S; Meyer, H; Offinger, J; Rehage, J; Rizk, A; Zaghloul, A, 2012
)
1.25
"Xylazine treatment induced significant decreases in HR, RR, MAP, insulin and NEFA concentrations, and Sao(2) and induced significant increases in glucose concentration."( Effects of xylazine hydrochloride on hormonal, metabolic, and cardiorespiratory stress responses to lateral recumbency and claw trimming in dairy cows.
Herdtweck, S; Meyer, H; Offinger, J; Rehage, J; Rizk, A; Zaghloul, A, 2012
)
1.49
"In xylazine-treated cats, yohimbine was an effective antagonist; arousal and walking occurred in an average of 2.8 minutes and 12.8 minutes, respectively."( Reversal of pentobarbital anesthesia with 4-aminopyridine and yohimbine in cats pretreated with acepromazine and xylazine.
Booth, NH; Clark, JD; Hatch, RC; Kitzman, JV; Zahner, JM, 1984
)
0.99
"Xylazine pretreatment also protected rats against electroshock-induced convulsions."( Pro and anticonvulsant effects of xylazine on convulsion models in rodents.
Bernardi, MM; Gorniak, SL; Palermo-Neto, J; Spinosa, FR; Spinosa, Hde S, 1994
)
1.29
"Xylazine treatments significantly and dose-dependently decreased the heart rate, respiratory rate and ruminal motility, and increased the rectal temperature when compared with pretreatment values."( Stimulation of food intake by xylazine in sheep.
al-Dabbagh, BK; Mohammad, FK; Wahed, RA, 1996
)
1.3
"Xylazine-treated camels had significantly lower values for RBC, hemoglobin, and packed cell volume, and significantly higher blood glucose concentrations."( Hematologic effects of xylazine when used for restraint of Bactrian camels.
Bush, M; Custer, R; Kennedy, S; Kramer, L, 1977
)
1.29
"Xylazine pretreatment did not alter the cortisol response to CRF, suggesting that xylazine must act centrally above pituitary level when blocking the cortisol response to transport."( Effects of xylazine on the stress response to transport in male goats.
Dobson, H; Jones, RS; Sanhouri, AA,
)
1.24
"In xylazine-treated dogs, the mean dosage of thiopental required to induce anesthesia was 4.8 mg/kg."( Reversal of thiopental-induced anesthesia by 4-aminopyridine, yohimbine, and doxapram in dogs pretreated with xylazine or acepromazine.
Brown, J; Clark, JD; Hatch, RC; Jernigan, AD; Wilson, RC, 1985
)
1
"treatment with xylazine or UK14304, two α2-adrenergic agonists, reduced neutrophil migration by 60%."( Prevention of neutrophil extravasation by α2-adrenoceptor-mediated endothelial stabilization.
Álvarez de La Rosa, D; Arce-Franco, M; Armas-González, E; Barreiro, O; Díaz-González, F; Domínguez-Luis, MJ; Feria, M; Herrera-García, AM; Machado, JD; Pec, MK; Sánchez-Madrid, F, 2014
)
0.74
"Treatment with xylazine or xylazine plus hyaluronidase resulted in less discomfort than treatment with lidocaine, as indicated by animal behavior."( Efficacy of caudal epidural injection of lidocaine, xylazine and xylazine plus hyaluronidase in reducing discomfort produced by electroejaculation in bulls.
Costa, DS; Derossi, R; Faria, FJ; Pagliosa, RC, 2015
)
1.01
"Treatment with xylazine produced a significant (P < 0.01), transient, dose-dependent reduction in ICP that was blocked by pretreatment with tolazoline."( Intracranial pressure reduction by a central alpha-2 adrenoreceptor agonist after subarachnoid hemorrhage.
McCormick, JM; McCormick, PW; Spetzler, RF; Zabramski, JM, 1993
)
0.63
"Treatment with xylazine was associated with an overall increased FSH (P less than 0.01) and LH (P less than 0.05) pulse frequency, compared with that observed during 12-h pretreatment periods."( Effect of administration of an alpha 2-adrenergic agonist, xylazine, on pulsatile gonadotrophin secretion in anoestrous horse mares.
Fitzgerald, BP; Mellbye, LB, 1988
)
0.86

Toxicity

ExcerptReferenceRelevance
"The goals of the study were to find a safe intraperitoneal injection anesthesia protocol for medium-duration surgery in mice (e."( Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth.
Arras, M; Autenried, P; Rettich, A; Rülicke, T; Spaeni, D, 2001
)
0.31
" We recommend KXA as a safe and reliable anesthetic for mice requiring a surgical plane of anesthesia."( Safety and efficacy of various combinations of injectable anesthetics in BALB/c mice.
Belicha-Villanueva, A; Buitrago, S; Martin, TE; Tetens-Woodring, J; Wilding, GE, 2008
)
0.35
" By early 2021, MADDS detected shifts in cocaine purity, alerted communities of a new toxic fentanyl analogue and a synthetic cannabinoid contaminant, and confirmed the increase of xylazine (a veterinary sedative) in Massachusetts."( Implementation and Uptake of the Massachusetts Drug Supply Data Stream: A Statewide Public Health-Public Safety Partnership Drug Checking Program.
Consigli, A; Del Pozo, B; Erowid, E; Erowid, F; Green, TC; Jarczyk, C; Michelson, L; Olson, R; Reilly, B; Ruiz, S; Thyssen, S; Wightman, R,
)
0.32

Pharmacokinetics

Pharmacokinetic data after IA administration resulted in some xylazine absorption (bioavailability equal to 58.1 mg/kg) We compared retroorbital and intravenous lateral tail vein injection of ketamine-xylazine with regard to preparation time, utility, tissue distribution and time to onset of euthanasia.

ExcerptReferenceRelevance
" The plasma concentration of ketamine was measured several times after administration of the drug and these data were used to develop a two-compartment pharmacokinetic model."( Pharmacokinetics of ketamine in the horse.
Hayton, WL; Kaka, JS; Klavano, PA, 1979
)
0.26
"1 mg/kg of xylazine from 2 manufacturers and the pharmacokinetic parameters calculated from the disposition curves."( Pharmacokinetics of xylazine in ponies: influence of yohimbine.
Dyer, DC; Hsu, WH; Lloyd, WE, 1987
)
0.99
"The pharmacokinetic disposition of xylazine hydrochloride is described after both intravenous and intramuscular injection of a single dose, in four domestic species: horse, cattle, sheep and dog, by an original high performance liquid chromatographic technique."( The pharmacokinetics of xylazine hydrochloride: an interspecific study.
Alvinerie, M; Garcia-Villar, R; Ruckebusch, Y; Toutain, PL, 1981
)
0.85
" Most lidocaine pharmacokinetic variables also differed between groups."( Influence of general anesthesia on pharmacokinetics of intravenous lidocaine infusion in horses.
Feary, DJ; Mama, KR; Thomasy, S; Wagner, AE, 2005
)
0.33
" The first-order elimination rate constant was significantly higher and elimination half-life and mean residence time were lower for S-ketamine after S-ketamine compared to R-/S-ketamine administration."( Stereoselective pharmacokinetics of ketamine and norketamine after racemic ketamine or S-ketamine administration in Shetland ponies sedated with xylazine.
Knobloch, M; Kronen, PW; Landoni, MF; Larenza, MP; Levionnois, OL; Schatzmann, U; Theurillat, R; Thormann, W, 2008
)
0.55
"To develop a means of euthanasia to support rapid time-course pharmacokinetic studies in mice, we compared retroorbital and intravenous lateral tail vein injection of ketamine-xylazine with regard to preparation time, utility, tissue distribution, and time to onset of euthanasia."( Euthanasia method for mice in rapid time-course pulmonary pharmacokinetic studies.
Chiang, PC; Heyde, BR; Hu, Y; Schoell, AR; Tung, DK; Weir, DE, 2009
)
0.55
" Venous blood samples were collected at strategic time points and plasma concentrations of alfaxalone were assayed using liquid chromatography-mass spectrometry (LC/MS) and analysed by noncompartmental pharmacokinetic analysis."( The pharmacokinetics and pharmacodynamics of the injectable anaesthetic alfaxalone in the horse.
Goodwin, WA; Keates, HL; Pasloske, K; Pearson, M; Ranasinghe, MG; Sauer, B, 2011
)
0.37
"To determine the pharmacokinetic parameters of xylazine, ketamine, and butorphanol (XKB) administered IM and sodium salicylate (SAL) administered PO to calves and to compare drug effects on biomarkers of pain and distress following sham and actual castration and dehorning."( Pharmacokinetics and physiologic effects of intramuscularly administered xylazine hydrochloride-ketamine hydrochloride-butorphanol tartrate alone or in combination with orally administered sodium salicylate on biomarkers of pain in Holstein calves followi
Baldridge, SL; Coetzee, JF; Dritz, SS; Gehring, R; Havel, J; Kukanich, B; Reinbold, JB, 2011
)
0.86
" The rate constant of elimination of both drugs was greatly decreased and the elimination half-life was significantly greater in old compared with young rats."( Pharmacokinetics of ketamine and xylazine in young and old Sprague-Dawley rats.
Beaudry, F; Carrier, D; Castel, A; Vachon, P; Veilleux-Lemieux, D, 2013
)
0.67
" Pharmacokinetic data after IA administration resulted in some xylazine absorption (bioavailability equal to 58."( A pharmacokinetic/clinical approach to postulate a local action of intra-articular xylazine administration in the horse: a preliminary study.
Bazzica, C; Cagnardi, P; Della Rocca, G; Di Salvo, A; Giontella, A; Nannarone, S, 2014
)
0.87
" Pharmacokinetic parameters (T1/2 and AUC) increased and drug clearance decreased with aging, which strongly suggests that drug exposure is associated with the physiological results."( Physiological, pharmacokinetic and liver metabolism comparisons between 3-, 6-, 12- and 18-month-old male Sprague Dawley rats under ketamine-xylazine anesthesia.
Beaudry, F; Burns, P; Giroux, MC; Hélie, P; Santamaria, R; Vachon, P, 2016
)
0.64
" Pharmacodynamic parameters were determined using PK-PD modeling."( Pharmacokinetic and pharmacodynamics of xylazine administered to exercised thoroughbred horses.
Arthur, RM; Kass, PH; Knych, HK; McKemie, DS; Stanley, SD, 2017
)
0.72
" For pharmacokinetic evaluation, blood samples were collected over 12 hours and serum samples were analysed by high performance liquid chromatography-mass spectrometry."( Pharmacokinetics and sedative effects of dexmedetomidine in dairy calves.
Boccardo, A; Cagnardi, P; Capolongo, F; Di Cesare, F; Lucatello, L; Pravettoni, D; Ravasio, G; Villa, R, 2017
)
0.46
" Serial venous blood samples were collected for quantification of xylazine and dexmedetomidine, and the pharmacokinetic parameters were calculated."( Pharmacokinetics and clinical effects of xylazine and dexmedetomidine in horses recovering from isoflurane anesthesia.
Allweiler, S; Almeida, DC; Baldo, CF; Guedes, A; Knych, H; Tucker, L; Wendt-Hornickle, E, 2020
)
1.06
" Characteristics of sedation and selected pharmacodynamic parameters were compared between groups using a non-parametric Mann-Whitney U test."( Xylazine or detomidine in dairy calves: a comparison of clinically relevant pharmacodynamic parameters under sedation.
Brehm, W; Gittel, C; Hillmann, A; Michaele, A; Roth, S; Wippern, M, 2021
)
2.06
"This preliminary clinical investigation of the pharmacokinetic behavior of the main metamizole (dipyrone) metabolites 4-methylaminoantipyrine (4-MAA) and 4-aminoantipyrine (4-AA) in calves undergoing umbilical surgery is part of an already published main study."( Pharmacokinetics of metamizole (dipyrone) as an add-on in calves undergoing umbilical surgery.
Baumgartner, C; Behrendt-Wippermann, M; Brandl, J; Feist, M; Fux, D; Metzner, M; von Thaden, A, 2022
)
0.72
" The measured pharmacodynamic variables were sedative and analgesic effects and the effect on ataxia and some physiological parameters."( Pharmacodynamics and pharmacokinetics of nalbuphine in xylazine‑sedated horses.
Gadallah, S; Hammad, A; Misk, T; Mourad, A; Sharshar, A; Thabet, N, 2022
)
0.97

Compound-Compound Interactions

The objective of this study was to compare intravenous (IV) xylazine and detomidine as sedatives in combination with midazolam and ketamine for induction of anaesthesia.

ExcerptReferenceRelevance
"A xylazine and butorphanol drug combination produced minimal and transient hemodynamic effects and no significant respiratory depression when administered to 6 healthy horses."( A new analgesic drug combination in the horse.
Muir, WW; Robertson, JT, 1983
)
0.99
"15 mg/kg) were administered subcutaneously in the rat in combination with KET (50 mg/kg), in the presence or not of YOH (2 mg/kg)."( Corneal toxicity of xylazine and clonidine, in combination with ketamine, in the rat.
Bordi, F; Casini, ML; Corubolo, C; Fehér, J; Fumagalli, E; Guidolin, D; Leone, MG; Mattioli, F; Romanelli, L; Saso, L; Tita, B,
)
0.45
"To determine the anesthetic dose and cardiopulmonary effects of xylazine hydrochloride when used alone or in combination with ketamine hydrochloride and evaluate the efficacy of yohimbine hydrochloride to reverse anesthetic effects in captive Axis deer."( Anesthesia induced by administration of xylazine hydrochloride alone or in combination with ketamine hydrochloride and reversal by administration of yohimbine hydrochloride in captive Axis deer (Axis axis).
Reddy, AP; Shivaji, S; Sontakke, SD; Umapathy, G, 2007
)
0.85
"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
)
0.75
"To evaluate the effects of methadone, administered alone or in combination with acepromazine or xylazine, on sedation and on physiologic values in dogs."( Effects of methadone, alone or in combination with acepromazine or xylazine, on sedation and physiologic values in dogs.
Bettini, CM; Campagnol, D; Choma, JC; Figueroa, CD; Monteiro, ER, 2008
)
0.8
" In all treatments body temperature decreased, this effect being more pronounced in dogs receiving methadone alone or in combination with acepromazine."( Effects of methadone, alone or in combination with acepromazine or xylazine, on sedation and physiologic values in dogs.
Bettini, CM; Campagnol, D; Choma, JC; Figueroa, CD; Monteiro, ER, 2008
)
0.58
" Greater sedation was achieved when methadone was used in combination with acepromazine or xylazine."( Effects of methadone, alone or in combination with acepromazine or xylazine, on sedation and physiologic values in dogs.
Bettini, CM; Campagnol, D; Choma, JC; Figueroa, CD; Monteiro, ER, 2008
)
0.8
"To investigate physiologic effects of electroacupuncture (EA) combined with xylazine administration in goats."( Physiologic effects of electroacupuncture combined with intramuscular administration of xylazine to provide analgesia in goats.
Chen, JG; Chen, X; Ding, MX; Ding, Y; Hu, CM; Liu, DM; Zhou, ZY, 2009
)
0.8
"To evaluate antinociceptive and selected effects associated with IM administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.84
" Procedures-Each llama received tiletamine-zolazepam (2 mg/kg) combined with either xylazine (0."( Physiologic and antinociceptive effects following intramuscular administration of xylazine hydrochloride in combination with tiletamine-zolazepam in llamas.
Doherty, TJ; Egger, CM; Elliot, SB; Seddighi, R; Whitlock, BK, 2013
)
0.84
"This study evaluated the use of the injectable anesthetic, alphaxalone, as a single agent and in combination with ketamine, xylazine, and morphine in the Chilean rose tarantula, Grammostola rosea."( The use of injectable alphaxalone as a single agent and in combination with ketamine, xylazine, and morphine in the Chilean rose tarantula, Grammostola rosea.
Gjeltema, J; Posner, LP; Stoskopf, M, 2014
)
0.83
"To evaluate the cardiopulmonary and sedative effects of xylazine alone or in combination with methadone, morphine or tramadol in sheep."( Sedative and cardiopulmonary effects of xylazine alone or in combination with methadone, morphine or tramadol in sheep.
Auckburally, A; Borges, LP; Cerejo, SA; de Carvalho, LL; de Mattos-Junior, E; Nishimura, LT; Villela, IO, 2016
)
0.95
" Each drug combination was mixed in the syringe and injected intravenously."( Sedative and cardiopulmonary effects of xylazine alone or in combination with methadone, morphine or tramadol in sheep.
Auckburally, A; Borges, LP; Cerejo, SA; de Carvalho, LL; de Mattos-Junior, E; Nishimura, LT; Villela, IO, 2016
)
0.7
" Fasted pigs rotationally received either no drug, a single intravenous administration of A or X, or A or X combined with ketamine (AK or XK, respectively), and plasma concentrations of glucose, lactate, non-esterified fatty acids (NEFA), triglycerides (TG), glucagon, insulin, and cortisol were determined for a 5-h period following administration."( Effects of general anesthesia with ketamine in combination with the neuroleptic sedatives xylazine or azaperone on plasma metabolites and hormones in pigs.
Brüssow, KP; Daş, G; Görs, S; Kanitz, E; Metges, CC; Vernunft, A; Weitzel, JM, 2016
)
0.66
" 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
)
0.89
" 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
)
0.93
"The objective of this study was to compare intravenous (IV) xylazine and detomidine as sedatives in combination with midazolam and ketamine for induction of anaesthesia in horses undergoing field castration."( Comparison of xylazine and detomidine in combination with midazolam/ketamine for field castration in Quarter Horses.
Bass, L; Damone, J; Mama, K; Rao, S; Smith, MC, 2020
)
1.16
"To compare the sedative effects of intramuscular xylazine alone or combined with levomethadone or ketamine in calves before cautery disbudding."( A comparison of sedative effects of xylazine alone or combined with levomethadone or ketamine in calves prior to disbudding.
Adam, M; Aho, R; Hänninen, L; Hokkanen, AH; Norring, M; Raekallio, M; Salla, K; Taponen, S, 2021
)
1.15
"5 years (January 2019-June 2021) of driving under the influence of drugs (DUID) and medico-legal death investigation (MDI) cases was investigated, including other drugs detected in combination with xylazine."( Xylazine: Pharmacology Review and Prevalence and Drug Combinations in Forensic Toxicology Casework.
Barbieri, EJ; Kacinko, SL; Logan, BK; Mohr, ALA, 2022
)
2.35

Bioavailability

All three enzymes enhanced the absorption rate of xylazine and ketamine determined by measurement of the concentration in the perfusate.

ExcerptReferenceRelevance
" All three enzymes enhanced the absorption rate of xylazine and ketamine determined by measurement of the concentration in the perfusate."( [Use of hyaluronic acid cleaving enzymes for absorption acceleration. Results of an in vitro study with xylazine and ketamine].
Gross, C; Kietzmann, M, 2006
)
0.8
"To evaluate if prior sedation with xylazine would influence the rate of absorption of D(+)-xylose in 6 normal Standardbred horses in a randomised cross-over study."( The effect of sedation on D(+)-xylose absorption tests in 6 normal horses.
Fintl, C; Ihler, CF, 2011
)
0.65
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A safe and effective dosage of xylazine-ketamine for Indian fox (Vulpes bengalensis) is reported. The dose-response curve for methoxamine, but not for Xylazine, was shifted to the left by the neuroleptic.

ExcerptRelevanceReference
"Urine volume, urine pH, and urine glucose concentration were monitored for up to 24 hours after physiological saline or one of two dosage levels (0."( Effects of xylazine hydrochloride on urine in cattle.
Hartsfield, SM; Nelson, DR; Rumore, CA; Thurmon, JC, 1978
)
0.65
" A minimal effective dosage of 90 mg/kg for ketamine and 10 mg/kg for xylazine provided satisfactory anesthesia in 92% of the subjects, without adverse effects on gestation or the fetuses."( Ketamine/xylazine anesthesia in the pregnant rat.
Stickrod, G, 1979
)
0.91
" The drug was found to be effective and safe for a wide range of ungulates and pachyderms and Burchell's zebra (Equus burchelli) did not react to expected dosage levels."( Immobilisation of free-ranging wild animals using a new drug.
De Vos, V, 1978
)
0.26
" The optimal dosage was higher for excited and socialized adults and lower for juveniles than for unexcited unsocialized adults."( Evaluation of xylazine for chemical restraint of captive arctic wolves.
Philo, LM, 1978
)
0.62
" Maximum blood glucose concentrations were reached approximately 40 minutes after dosing and did not start to fall until 185 minutes."( The effect of xylazine upon hepatic glucose production and blood flow rate in the lactating dairy cow.
Symonds, HW, 1976
)
0.62
" Other than the prolongation of immobilization at dosages larger than or equal to 3 mg/kg, these times were not significantly affected by dosage or sex of the deer."( Xylazine as an immobilizing agent for captive white-tailed deer.
Roughton, RD, 1975
)
1.7
" 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
)
0.51
" Further investigations need to be done to establish the most appropriate dosage rates for these preparations in ostriches."( Ostrich (Struthio camelus) immobilisation using carfentanil and xylazine and reversal with yohimbine and naltrexone.
Malan, JH; Quandt, SK; Raath, JP, 1992
)
0.52
") caused a 20-30 fold rightward displacement of the dose-response curve to xylazine, but did not affect responses to B-HT933."( Alpha 2-adrenoceptor blocking profile of SK&F 104078: further evidence for receptor subtypes.
Akers, I; Coates, J; Drew, GM; Sullivan, AT, 1991
)
0.51
" Drowsiness was found in calves given the lowest dosage of atipamezole (3 micrograms/kg) after the calves stood."( Antagonistic effect of atipamezole on xylazine-induced sedation, bradycardia, and ruminal atony in calves.
Hsu, WH; Kersting, KW; Thompson, JR, 1991
)
0.55
" Examination under xylazine hydrochloride at either dosage yielded a change in median laryngeal grade from the unsedated examination in 45% of the evaluations."( The reliability of endoscopic examination in assessment of arytenoid cartilage movement in horses. Part II. Influence of side of examination, reexamination, and sedation.
Ducharme, NG; Erb, HN; Fubini, SL; Hackett, RP,
)
0.46
" When YOH was used as an anesthetic antagonist at dosage of 20 mg/kg, 20% mortality was observed and was attributable to acute respiratory arrest."( Antagonism of ketamine-xylazine anesthesia in rats by administration of yohimbine, tolazoline, or 4-aminopyridine.
Komulainen, A; Olson, ME, 1991
)
0.59
" The above parameters as well as mean arterial blood pressure, righting, palpebral, pedal, and jaw reflexes were monitored ten minutes after the intramuscularly administered dosage and throughout 4 hours of infusion."( The effects of prolonged ketamine-xylazine intravenous infusion on arterial blood pH, blood gases, mean arterial blood pressure, heart and respiratory rates, rectal temperature and reflexes in the rabbit.
Richardson, ME; Scott, RA; Wyatt, JD, 1989
)
0.56
" The dose-response curve for methoxamine, but not for xylazine, was shifted to the left by the neuroleptic."( Increased peripheral alpha 1-adrenoceptor sensitivity following chronic thioridazine treatment in the pithed rat.
Badia, A; Cuffí, ML; Vila, E, 1989
)
0.53
" Using a dosage of 3-5 mg/kg there is a marked negative effect on the cardio-vascular system."( [The antagonism of ketamine/xylazine anesthesia ("Hellabrunn mixture") in wild zoo ruminants].
Erhardt, W; Hafner, S; Halm, S; von Hegel, G; Wiesner, H, 1989
)
0.57
" With the exception of a greater hypertensive response, detomidine at the dosages studied, produced cardiovascular effects that were very similar to those of the recommended dosage of xylazine."( Cardiovascular effects of detomidine, a new alpha 2-adrenoceptor agonist, in the conscious pony.
Garner, HE; Krause, GF; Sarazan, RD; Starke, WA, 1989
)
0.47
" To investigate the role of systemic absorption in the production of epidural analgesia, the previously utilized epidural xylazine dosage was given intramuscularly to four adult cows."( Caudal epidural analgesia in cattle using xylazine.
Caron, JP; LeBlanc, PH, 1989
)
0.75
"The systemic administration of an anesthetic dosage of a combination of xylazine and ketamine hydrochloride produced an acute exposure keratopathy which progressed into a syndrome resembling keratoconjunctivitis sicca."( Keratoconjunctivitis sicca with associated secondary uveitis elicited in rats after systemic xylazine/ketamine anesthesia.
Fox, A; Kufoy, EA; Pakalnis, VA; Parks, CD; Wells, A; Yang, CH, 1989
)
0.73
" Idazoxan given at a dosage of 30 micrograms/kg also reversed xylazine-induced bradycardia."( Antagonistic effect of idazoxan on xylazine-induced central nervous system depression and bradycardia in calves.
Hsu, WH; Kersting, KW; Thompson, JR, 1989
)
0.79
" According to published data and past experience, the dosage of xylazine used would be expected to provide 115, 120, and 100 minutes of immobilization in captive moose, mule deer, and white-tailed deer, respectively."( Use of yohimbine and 4-aminopyridine to antagonize xylazine-induced immobilization in North American Cervidae.
Olsen, CD; Renecker, LA, 1985
)
0.76
") gave a small parallel shift in the noradrenaline log dose-response curve and prevented the reduction in the maximum response by subsequent administration of xylazine."( Interactions between noradrenaline and alpha 2-adrenoceptor agonists in the superior mesenteric arterial bed of the rat.
Hiley, CR; Nichols, AJ; Thomas, GR, 1986
)
0.47
"Ten dogs were studied to determine the effects of xylazine, ketamine, and xylazine combined with ketamine on the dosage of epinephrine required to produce ventricular arrhythmia."( Effects of xylazine and ketamine on epinephrine-induced arrhythmia in the dog.
Heath, RB; Wingfield, WE; Wright, M,
)
0.77
" The dose-response curve of detomidine was shifted to the right in a parallel manner by the selective alpha 2-antagonist idazoxan."( Effect of detomidine on the release and turnover of noradrenaline in rat brain.
Kaisila, M; MacDonald, E; Virtanen, R, 1986
)
0.27
" After administration of glycopyrrolate, cardiac performance decreased, but the decrease was not significant when compared with the ventricular performance of the cats after administration of the large dosage of xylazine."( Cardiac performance in cats after administration of xylazine or xylazine and glycopyrrolate: echocardiographic evaluations.
Dunkle, N; Moise, NS; Scarlett-Kranz, J; Short, CE, 1986
)
0.71
" Dose-response curves in group 1 indicated a biphasic response to the drug with vasoconstriction, increased motility, and increased oxygen consumption at lower doses followed by a return toward base-line values at higher doses."( Effects of xylazine on equine intestinal vascular resistance, motility, compliance, and oxygen consumption.
Arden, WA; Chou, CC; Derksen, FJ; Stick, JA, 1987
)
0.66
" The dosage rates of the immobilization combinations for mammmals, birds and reptiles are presented in tabular form."( [Practical advice concerning the immobilization of wild and zoo animals].
von Hegel, G; Wiesner, H, 1985
)
0.27
" Yohimbine injection at postpentobarbital dosing minute 50 reversed the resumed xylazine-induced bradycardia and relieved other signs of respiratory depression associated with xylazine-pentobarbital anesthesia."( Xylazine-pentobarbital anesthesia in dogs and its antagonism by yohimbine.
Hsu, WH, 1985
)
1.94
"Ketamine, ketamine-xylazine, and ketamine-diazepam were evaluated clinically in 15 ferrets, and safe dosage was determined for each."( Evaluation of ketamine, ketamine-xylazine and ketamine-diazepam anesthesia in the ferret.
Glaser, C; Moreland, AF, 1985
)
0.88
"Twenty-four crossbred steers (4 groups of 6 steers each) were injected IM with a standard dosage range of xylazine hydrochloride (0."( Antagonism of xylazine sedation by 4-aminopyridine and yohimbine in cattle.
Booth, NH; Hatch, RC; Kitzman, JV; Wallner, B, 1982
)
0.84
" In contrast, the dose-response curves to tiamenidine and clonidine were flatter and bell-shaped with maxima of 30 and 60 min, respectively."( Sleeping times evoked by alpha adrenoceptor agonists in two-day-old chicks: an experimental model to evaluate full and partial agonists at central alpha-2 adrenoceptors.
Cavero, I; Doxey, JC; Roach, AG; Strachan, DA, 1983
)
0.27
" Because of the narrow range for safe dosage for Fentaz the use of Rompun for immobilizing deer is recommended."( The effect of immobilizing drugs on adrenal responsiveness to ACTH in Rusa deer.
Stelmasiak, T; Van Mourik, S, 1984
)
0.27
" Hypotensive potency after intravenous administration to anesthetized, normotensive rats was determined as a measure of central alpha-adrenergic activity and expressed as pC25, obtained from log dose-response curves."( Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
de Jonge, A; Lam, E; Slothorst-Grisdijk, FP; Timmermans, PB; van Meel, JC; van Zwieten, PA, 1981
)
0.26
" Our data indicate that yohimbine produces a significant reversal of xylazine-induced rumen hypomotility at dosage levels that are without effect on sedation induced by this drug."( Influence of yohimbine on xylazine-induced depression of central nervous, gastrointestinal and cardiovascular function in the calf.
Guard, CL; Schwark, WS, 1984
)
0.8
"Groups of fasted atropinized crossbred dogs of both sexes were injected IM with a standard dosage of a xylazine-acepromazine combination (2."( Acepromazine-xylazine combination in dogs: antagonism with 4-aminopyridine and yohimbine.
Booth, NH; Brown, J; Cronin, MF; Hatch, RC, 1983
)
0.85
" Intravenous injection of xylazine (1 to 10 mg/kg) induced a dose-dependent CNS depression that was prevented by a low dosage of yohimbine (0."( Effect of yohimbine on xylazine-induced central nervous system depression in dogs.
Hsu, WH, 1983
)
0.88
" Particular attention was focused on the establishment of an LD50 and the development of a dose-response curve."( Evaluation of ketamine/xylazine anesthesia in the guinea pig: toxicological parameters.
D'Alleinne, CP; Mann, DD, 1982
)
0.57
" The use of the newly developed piperidine derivative R 33799 at weight treated dosage levels can be strongly recommended for the immobilisation of hartebeest."( On the immobilization of hartebeest and kob in Upper Volta.
Dräger, N; Küpper, W; Mehlitz, D; Zillmann, U, 1981
)
0.26
" The low dosage in cattle did not permit calculation."( The pharmacokinetics of xylazine hydrochloride: an interspecific study.
Alvinerie, M; Garcia-Villar, R; Ruckebusch, Y; Toutain, PL, 1981
)
0.57
" When xylazine was used at the same dosage in 13 clinical cases involving surgery of short duration, it proved to be a satisfactory sedative, analgesic, and muscle relaxant."( Evaluation of xylazine in camels.
Nigam, JM; Peshin, PK; Robinson, BA; Singh, SC, 1980
)
1.1
" Although it was possible that the clinical findings in these horses may have resulted from use of an inadequate dosage of carfentanil or xylazine, or both, analysis of the results more likely indicated that domestic and exotic horses may respond differently to carfentanil, and domestic horses may not be a good model for use in studies of carfentanil."( Complications with the use of carfentanil citrate and xylazine hydrochloride to immobilize domestic horses.
Carpenter, JW; Leith, DE; Shaw, ML, 1995
)
0.74
" 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
)
0.53
" 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
)
0.53
" Regional extension of anaesthesia was comparable after dosing with xylazine and lidocaine (tail, after, vulva and perineum)."( [Experiences with the use of xylazine for sacral epidural anesthesia in cattle].
Kehler, W; Rehage, J; Scholz, H, 1994
)
0.82
" Reversal with yohimbine hydrochloride using a mean dosage of 83 mg/animal resulted in a mean (SD) recovery time of 22."( Postpartum immobilization of adult female moose using xylazine, ketamine and yohimbine hydrochlorides.
Addison, EM; Garner, DL, 1994
)
0.54
"The cardiorespiratory effects of thiamylal (10 mg/kg of body weight, IV) and the effects of preanesthetic medication with diazepam, acepromazine, detomidine, or xylazine administered prior to a thiamylal dosage of 6 mg/kg, IV, were evaluated in 6 adult horses."( Effects of diazepam, acepromazine, detomidine, and xylazine on thiamylal anesthesia in horses.
Mason, DE; Muir, WW, 1993
)
0.73
"kg-1) shifted the dose-response curve of xylazine induced sedation to the right, hemicholinum-3 (3 micrograms icv), which inhibits the synthesis of acetylcholine, shifted the dose-response curve to the left."( [Antagonistic effects of cholinergic drugs on xylazine induced sedation].
Ding, RG; Huang, SJ; Yang, JS, 1993
)
0.81
" Two dosage levels were administered intraperitoneally."( Evaluation of ketamine-xylazine in Syrian hamsters.
Clark, JA; Dixon, D; Forsythe, DB; Myers, PH; Payton, AJ; Snipe, JR, 1993
)
0.6
" Recovery time varied with weight and dosage of yohimbine."( Immobilization of Rocky Mountain elk with Telazol and xylazine hydrochloride, and antagonism by yohimbine hydrochloride.
Brundige, GC; Hustead, DR; Jenks, JA; Millspaugh, JJ; Tyner, CL, 1995
)
0.54
" Eleven muskrats were intramuscularly injected using a high (n = 7) or low (n = 4) dosage of a 20:1 mixture of ketamine (12 or 20 mg) and xylazine (0."( Immobilization of muskrats (Ondatra zibethicus) with ketamine and xylazine.
Belant, JL, 1996
)
0.73
" The idazoxan dose-response curve for this suppression of fentanyl antinociception assessed with tail flick latency was the same as that for suppression of xylazine."( Antinociceptive actions of intrathecal xylazine: interactions with spinal cord opioid pathways.
Davies, A; Gent, JP; Goodchild, CS; Guo, Z, 1996
)
0.76
" Intramuscular xylazine appears to be an effective analgesic agent for acute pain in the sheep and further investigation into ideal administration regimens and dosage may provide more detailed information on relationships between dose, analgesic and sedative effects."( Efficacy of intra-muscular analgesics for acute pain in sheep.
Grant, C; Kuchel, TR; Upton, RN, 1996
)
0.65
" The dosage based on experimental studies."( [Clinical investigations of an i.m. combination anesthesia with fentanylclimazolam/xylazine and postoperative i.v. antagonism with naloxone/sarmazenil/yohimbine in guinea pigs].
Brill, T; Erhardt, W; Henke, J; Lendl, C; Matis, U; Otto, K; Roberts, U, 1996
)
0.52
" Higher dosage of yohimbine inhibited the baseline expression of bFGF."( Alpha 2-adrenergic agonists induce basic fibroblast growth factor expression in photoreceptors in vivo and ameliorate light damage.
Cao, W; Cheng, T; Li, Y; Steinberg, RH; Wen, R, 1996
)
0.29
" The addition of methoxyflurane significantly potentiated the anaesthetic and analgesic properties of the high dosage ketamine-xylazine combination."( Evaluation of anaesthetic regimens in guineapigs.
Crenshaw, D; Hinson, A; Radde, GR; Toth, LA, 1996
)
0.5
" Then a higher xylazine dosage was given after the 15-minute measurements were taken."( Actions of xylazine in young swine.
Castillo-Olivares, JL; Gómez de Segura, IA; Mascías, A; Santos, M; Steffey, EP; Tendillo, FJ, 1997
)
1.04
"Xylazine did not induce adequate sedative or analgesic effects in pigs at any dosage tested; however, cardiovascular effects were considerable."( Actions of xylazine in young swine.
Castillo-Olivares, JL; Gómez de Segura, IA; Mascías, A; Santos, M; Steffey, EP; Tendillo, FJ, 1997
)
2.13
"The carfentamil-xylazine combination at the dosage used induced hypoxemia, pronounced arterial hypertension, and significant increase in plasma norepinephrine and decrease in plasma 3,4-dihydroxyphenylacetic acid concentrations in bongo antelopes."( Effects of a carfentanil-xylazine combination on cardiopulmonary function and plasma catecholamine concentrations in female bongo antelopes.
Citino, SB; Dawson, R; Schumacher, J, 1997
)
0.95
" 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
)
0.53
" Skunks were immobilized with a mean (+/- SD) dosage of 15."( Field immobilization of pygmy spotted skunks from Mexico.
Cantú Salazar, L; Casariego Madorell, MA; De Villa Meza, A; González-Romero, A; Hidalgo Mihart, MG; Laundré, JW; López González, CA; Martínez Meyer, E, 1998
)
0.3
" Dosage (mg/kg of body weight) of xylazine received, induction time, and recovery time after handling did not differ among sex-age classes."( Immobilization of mountain goats with xylazine and reversal with idazoxan.
Côté, SD; Festa-Bianchet, M; Haviernick, M, 1998
)
0.85
" The participation of alpha2-adrenergic receptors in the sedative effect provoked by amitraz was studied by dosing yohimbine (0."( Characterization of the antinociceptive and sedative effect of amitraz in horses.
Carregaro, AB; Gonçalves, SC; Harkins, JD; Mataqueiro, MI; Queiroz-Neto, A; Tobin, T; Zamur, G, 1998
)
0.3
" These findings support the use of xylazine as an effective analgesic in sheep with comparable effects and consistent dosing requirements per unit body weight between adult sheep and lambs."( The anti-nociceptive efficacy of low dose intramuscular xylazine in lambs.
Grant, C; Upton, RN, 2001
)
0.83
"The minimal changes to cardiovascular and respiratory values in this study verify the safety of previously suggested analgesic dosing regimens for sheep."( Cardiovascular and haemodynamic effects of intramuscular doses of xylazine in conscious sheep.
Grant, C; Upton, RN, 2001
)
0.55
"Of the 5,766 cats for which dosing records were complete, 4,584 (79."( Use of the anesthetic combination of tiletamine, zolazepam, ketamine, and xylazine for neutering feral cats.
Centonze, LA; Cistola, AM; Levy, JK; Robertson, SA; Williams, LS, 2002
)
0.55
"0 min after the intravenous administration of each drug and at all dosages except the lowest dosage of atropine."( Ultrasonographic evaluation of reticular motility in cows after administration of atropine, scopolamine and xylazine.
Braun, U; Gansohr, B; Haessig, M, 2002
)
0.53
" The mean dosage (0."( Tiletamine-zolazepam, ketamine, and xylazine anesthesia of captive cheetah (Acinonyx jubatus).
Bonar, CJ; Evans, SE; Lewandowski, AH, 2002
)
0.59
" Although induction time was similar between drugs, induction dosage and volume were less with XZT."( Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine.
Cattet, MR; Caulkett, NA; Lunn, NJ, 2003
)
0.6
"Compared to other laboratory animals, little is known about the use of anesthetics in birds, potentially resulting in the use of improper dosing regimens."( Lack of efficacy of injectable ketamine with xylazine or diazepam for anesthesia in chickens.
Broderson, JR; Clifton, KR; Poulos, S; Varner, J; Wyatt, RD, 2004
)
0.58
" We assessed the suitable dosage of narcotics and its correlation to severe respiratory adverse events in 269 cases of ketamine/xylazine anesthesia in male Wistar rats for performance of magnetic resonance imaging after middle cerebral artery occlusion (MCAO) or sham surgery."( Ketamine/xylazine anesthesia for radiologic imaging of neurologically impaired rats: dose response, respiratory depression, and management of complications.
Dittmar, MS; Fehm, NP; Horn, M; Vatankhah, B, 2004
)
0.95
"Anesthesia has an influence on the disposition of lidocaine in horses, and a change in dosing during anesthesia should be considered."( Influence of general anesthesia on pharmacokinetics of intravenous lidocaine infusion in horses.
Feary, DJ; Mama, KR; Thomasy, S; Wagner, AE, 2005
)
0.33
" A combination of 500 mg zolazepam, 500 mg tiletamine, 500 mg xylazine, and 1000 mg (10 ml) ketamine, administered in a dosage of 1 ml per 100-150 kg bodyweight (depending on the species), proved to be most reliable and effective."( [Immobilization of cattle and bison with a combination of xylazine, zolazepam-tiletamine and ketamine].
Hofkes, LM; Hoyer, MJ; Overgaauw, PA; van Dijk, P, 2005
)
0.81
" A fixed ratio of 1 mg CAR:10 mg XYL intramuscularly was used, increasing or decreasing the dosage until the optimal dosage (defined by an induction time < 3 min and PaCO(2)< 60 mmHg) was reached for each animal."( Determination and evaluation of an optimal dosage of carfentanil and xylazine for the immobilization of white-tailed deer (Odocoileus virginianus).
Miller, KV; Osborn, DA; Ramsay, EC; Schumacher, J; Storms, TN; Zagaya, N, 2005
)
0.56
"01) between dosage and time to first effect of immobilants."( Tiletamine-zolazepam-xylazine immobilization of American marten (Martes americana).
Belant, JL, 2005
)
0.65
" Recommendation on dosage are given."( Experience with drugs for capture and restraint of wildebeest, impala, eland and hartebeest in Kenya.
Drevemo, SA; Grootenhuis, JG; Karstad, L, 1976
)
0.26
"Using a crossover design, the effects of the addition of ketamine to a previously determined optimal hand-injected immobilization dosage of carfentanil/xylazine were evaluated in 11 adult white-tailed deer (Odocoileus virginianus)."( Effects of ketamine on carfentanil and xylazine immobilization of white-tailed deer (Odocoileus virginianus).
Miller, KV; Osborn, DA; Ramsay, EC; Schumacher, J; Storms, TN, 2006
)
0.8
" To explore the optimal KX dosage and observation time for murine echocardiography, we compared the effects of various KX combinations on echocardiographic measurement."( Optimizing dosage of ketamine and xylazine in murine echocardiography.
Dart, AM; Du, XJ; Ming, Z; Xu, Q,
)
0.41
"Three series of trials involving 10 domestic short-haired cats were carried out to determine the influence of dosage of contrast media or type of chemical restraint on feline excretory urography."( Influence of dosage and chemical restraints on feline excretory urography.
Adetunji, A; Ajadi, RA; Okoh, JU; Omoerah, VO, 2006
)
0.33
" There was no relationship between the amount (mg/kg) of Telazol-xylazine injected and time to first effect of immobilants, dosage and time to induction, or between dosage and time to recovery."( Tiletamine-zolazepam-xylazine immobilization of fishers (Martes pennanti).
Belant, JL, 2007
)
0.9
" At 10(-7) M of ST-91, the antagonism was characterized by a rightward shift of isoproterenol dose-response curve (A50=6."( alpha2B-adrenoceptor agonist ST-91 antagonizes beta2-adrenoceptor-mediated relaxation in rat mesenteric artery rings.
Gyires, K; Kató, E; Lipták, L; Mátyus, P; Rónai, AZ; Shujaa, N, 2008
)
0.35
"The influence of increasing the dosage of ketamine on anaesthesia induced by a combination of ketamine, xylazine and midazolam in pigs was determined by assessing the onset of action (OAN), duration of analgesia (DAN), anaesthesia time (ANT), and recovery time (RCT) in 10 growing pigs (Mean weight: 18."( Increasing ketamine dose enhances the anaesthetic properties of ketamine-xylazine-midazolam combinations in growing pigs.
Adeleye, OE; Ajadi, RA; Makinde, AF; Smith, OF, 2008
)
0.79
" ZL-n-91 (3 microg, 10 microg, 30 microg kg(-1)) dose-dependently reduced the total leukocyte number, neutrophil number and total protein content in BALF, MPO activity, TNF-alpha level and cAMP-PDE, PDE4 activity in lung homogenate, but the effect of ZL-n-91 in pathological changes and lung wet w/d ratio is slight; Rol and Dex significantly reduced lung wet w/d ratio and improved pathological changes, neutrophil around the pulmonary vessel and airway significantly reduced, symptoms of lung edema relieved; The PH value, P(a)O(2) and P(a)CO(2) in ZL-n-91 high dosage group and Rol group had changes, but there was no significant difference compared with LPS group or saline group; After the administration, the righting reflex recovery time significantly shorten in every group of ZL-n-91."( Action of a Novel PDE4 inhibitor ZL-n-91 on lipopolysaccharide-induced acute lung injury.
Chen, JQ; Liang, YQ; Lu, JJ; Mao, LG; Tang, HF; Tang, JF; Wang, XF; Wang, YJ; Zheng, X, 2010
)
0.36
" Prior treatment with each dosage of metoclopramide significantly reduced the frequency of emetic episodes (P<0."( Effects of metoclopramide on emesis in cats sedated with xylazine hydrochloride.
Jarolmasjed, S; Kolahian, S, 2010
)
0.61
"Administration of a subanesthetic dosage of ketamine with xylazine and butorphanol may facilitate certain procedures, such as insertion of a dental float, in horses and enhance tolerance to pressure stimulation, but it may worsen responses to acute pain, such as that caused by a needle prick."( Evaluation of sedation and analgesia in standing horses after administration of xylazine, butorphanol, and subanesthetic doses of ketamine.
Contino, EK; Ferris, DJ; Kawcak, CE; Mama, KR; Wagner, AE, 2011
)
0.84
"The purpose of this study was to examine the effects of a clinically relevant opioid on the production of augmented breaths (ABs) in unanesthetized animals breathing normal room air, using a dosage which does not depress breathing."( The "other" respiratory effect of opioids: suppression of spontaneous augmented ("sigh") breaths.
Azubike, E; Bell, HJ; Haouzi, P, 2011
)
0.37
" Skunks were immobilized with a mean (±SD) dosage of 24."( Field immobilization of Molina's hog-nosed skunk (Conepatus chinga) using ketamine and xylazine.
Casanave, EB; Castillo, DF; Lucherini, M; Vidal, EL, 2012
)
0.6
" In this report we have used the murine model of tularemia, with Francisella tularensis live vaccine strain (FTLVS) infection, to evaluate the efficiency of pneumonic delivery via intranasal dosing performed either with differing instillation volumes or different types of anesthesia."( Visualization of murine intranasal dosing efficiency using luminescent Francisella tularensis: effect of instillation volume and form of anesthesia.
Bina, JE; Bina, XR; Fabrizio, TP; Miller, MA; Parvathareddy, J; Stabenow, JM; Wodowski, AJ; Zalduondo, L, 2012
)
0.38
" The dosage of 5 mg ketamine/kg body mass was rarely sufficient to obtain surgical tolerance in group INJE."( [Comparison of three different anesthesia procedures in calves with respect to possible pain-associated reactions].
Hefti, A; Metzner, M; Sauter-Louis, C; Schlemmer, I,
)
0.13
" A safe and effective dosage of xylazine-ketamine for Indian fox (Vulpes bengalensis) is reported, based on 37 wild Indian fox immobilizations between April 2006 and May 2007."( Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of Indian fox (Vulpes bengalensis) in field situations.
Belsare, AV; Vanak, AT, 2013
)
1.13
" Les chats dans les autres groupes reçurent de la xylazine par voie intramusculaire à un dosage de 2 mg/kg de poids corporel (PC), et de la saline (comme témoin); 160 μg/kg PC de prazosin; ou 40, 160, ou 480 μg/kg PC d’atipamezole ou de yohimbine par voie intraveineuse 0,5 h plus tard."( Antagonistic effects of atipamezole, yohimbine, and prazosin on xylazine-induced diuresis in clinically normal cats.
Hikasa, Y; Miki, Y; Murahata, Y, 2014
)
0.89
" The time of year, most likely associated with differences in ambient temperature and in confinement, influenced the recommended dosage for xylazine and tiletamine-zolazepam in fallow deer."( Influence of Ambient Temperature and Confinement on the Chemical Immobilization of Fallow Deer ( Dama dama ).
Costa, GL; Cucinotta, G; Interlandi, C; Morici, M; Musicò, M; Nastasi, B; Spadola, F, 2017
)
0.66
" Although atipamezole and yohimbine dosing guidelines are available for mice, no controlled comparison has been performed to guide the lab animal community in the selection of one over the other."( Comparison of Atipamezole with Yohimbine for Antagonism of Xylazine in Mice Anesthetized with Ketamine and Xylazine.
Janssen, CF; Kracinovsky, KB; Maiello, P; Newsome, JT; Wright, MJ, 2017
)
0.7
" La narcose des rennes représente un défi particulier car le dosage sûr et efficace des anesthésiques et trop peu connu."( Challenging anaesthetic management of captive reindeer (Rangifer tarandus): Report of 4 cases.
Adami, C; McSloy, A; Monticelli, P; Morath, U, 2017
)
0.46
" The projected method was practiced successfully to the dosage form and spiked serum."( Highly Sensitive Voltammetric Sensor Using Carbon Nanotube and an Ionic Liquid Composite Electrode for Xylazine Hydrochloride.
El-Shal, MA; Hendawy, HAM, 2019
)
0.73
"To determine the effective dosage of the combination tiletamine-zolazepam-ketamine-xylazine (TKX), with or without methadone, in dogs."( Determination of the effective dosage of tiletamine-zolazepam-ketamine-xylazine, with or without methadone, in dogs.
Baier, ME; Herrera Becerra, JR; Martins, LGB; Monteiro, ER; Souza, MJ, 2022
)
1.18
" Here, we present dosage regimens of ketamine/xylazine/atropine in 10-day-old C57BL/6J mouse pups that allow endotracheal intubation, while minimizing animal mortality."( Anesthesia and Intubation of Preadolescent Mouse Pups for Cardiothoracic Surgery.
Feneley, MP; Graham, RM; Iismaa, SE; Nicks, AM; Skowno, JJ; Wu, J, 2022
)
0.98
"The present study aimed to find the optimal dosage of K-X and its association with the changes in dendritic spine number of the CA1 region for aged and young rats of both sexes."( Optimisation of ketamine-xylazine anaesthetic dose and its association with changes in the dendritic spine of CA1 hippocampus in the young and old male and female Wistar rats.
Namavar, MR; Sotoudeh, N, 2022
)
1.02
" The doses or dosing intervals of antimicrobials administered to horses undergoing anesthesia may need to be adjusted to ensure maintenance of safe and effective plasma concentrations."( Potassium penicillin and gentamicin pharmacokinetics in healthy conscious and anesthetized horses.
Bogers, SH; Council-Troche, RM; Davis, JL; Wilson, KE, 2023
)
0.91
" At the first change the xylazine dosage was the same for surgery, and sequentially the dosage could be reduced (0."( [Sole abscess (Pododermatitis purulenta superficialis) in a Bactrian camel - diagnosis, treatment, and healing process].
Eibl, C; Kofler, J; Schoiswohl, J, 2023
)
1.21
" Consistent pulmonary delivery is critical for experimental power and reproducibility, but we observed variation in outcomes between handlers using different anesthetic approaches for intranasal dosing in mice."( Optimizing anesthesia and delivery approaches for dosing into lungs of mice.
Cleary, SJ; Conrad, C; Looney, MR; Magnen, M; Moussavi-Harami, SF; Qiu, L; Seo, Y, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
emeticAny agent that induces nausea and vomiting.
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
sedativeA central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
[role 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]

Drug Classes (3)

ClassDescription
methylbenzeneAny alkylbenzene that is benzene substituted with one or more methyl groups.
1,3-thiazine
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
[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 (35)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency2.11540.003245.467312,589.2998AID2517
SMAD family member 2Homo sapiens (human)Potency10.68220.173734.304761.8120AID1346859
SMAD family member 3Homo sapiens (human)Potency10.68220.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency24.84460.000811.382244.6684AID686978; AID686979
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926; AID938
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.00700.000214.376460.0339AID720691
cytochrome P450 2D6Homo sapiens (human)Potency15.48710.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency100.00000.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency2.68551.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency24.90530.00207.533739.8107AID891
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency37.93300.134610.395030.1313AID1347049
ras-related protein Rab-9AHomo sapiens (human)Potency3.54810.00022.621531.4954AID485297
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.00000.00798.23321,122.0200AID2551
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency0.01000.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency13.34770.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.79430.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency0.01001.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (86)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID36785Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 1.4*10e-71984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID33252Peripheral hypertensive activity in pithed normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID23715Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID23716Partition coefficient (logD7.4)1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID197167Hypotensive activity (25% decrease in arterial pressure) after i.v. administration to anesthetized normotensive rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID33250Central hypotensive activity in anesthetized normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID36723Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 6.1*10e-51984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1998Biochemical pharmacology, Apr-01, Volume: 55, Issue:7
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,887)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990555 (29.41)18.7374
1990's399 (21.14)18.2507
2000's365 (19.34)29.6817
2010's390 (20.67)24.3611
2020's178 (9.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.99

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 Index91.99 (24.57)
Research Supply Index7.69 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index168.92 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (91.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials207 (10.45%)5.53%
Reviews35 (1.77%)6.00%
Case Studies68 (3.43%)4.05%
Observational2 (0.10%)0.25%
Other1,669 (84.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]