Epinephrine
From DrugPedia: A Wikipedia for Drug discovery
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|log P (octanol-water) | |log P (octanol-water) | ||
| - | |-1.37E+00 | + | |(-1.37E+00) |
| - | |(none) | + | |(none) |
| + | | | ||
|EXP | |EXP | ||
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Revision as of 08:49, 5 November 2008
Epinephrine Pubchem(5816)
The active sympathomimetic hormone from the adrenal medulla in most species. It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. It is used in asthma and cardiac failure and to delay absorption of local anesthetics.
KEGG Pathway(C00788,D00095)
- Tyrosine metabolism
- Neuroactive ligand-receptor interaction
Target
- alpha1a-adrenergic receptor agonist
- alpha1b-adrenergic receptor agonist
- alpha1d-adrenergic receptor agonist
- alpha2a-adrenergic receptor agonist
- alpha2b-adrenergic receptor agonist
- alpha2c-adrenergic receptor agonist
- beta1-adrenergic receptor agonist
- beta2-adrenergic receptor agonist
- beta3-adrenergic receptor agonist
Activity Adrenergic [vasoconstrictor]
| Physical Property | Value | Units | Temp (deg C) | Source |
|---|---|---|---|---|
| Melting Point | 211.5 | deg C | EXP | |
| pKa Dissociation Constant | 8.59 | (none) | 25 | EXP |
| log P (octanol-water) | (-1.37E+00) | (none) | EXP | |
| Water Solubility | 180 | mg/L | 20 | EXP |
| Vapor Pressure | 7.37E-07 | mm Hg | 25 | EST |
| Henry's Law Constant | 7.06E-19 | atm-m3/mole | 25 | EST |
| Atmospheric OH Rate Constant | 1.38E-10 | cm3/molecule-sec | 25 | EST |
Organism Test Type Route Reported Dose (Normalized Dose) Effect Source |cat |LDLo |intravenous |500ug/kg (0.5mg/kg) | |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |cat |LDLo |subcutaneous |20mg/kg (20mg/kg) | |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |dog |LD50 |intravenous |100ug/kg (0.1mg/kg) | |Drugs in Japan Vol. 6, Pg. 120, 1982. |- |dog |LD50 |subcutaneous |5mg/kg (5mg/kg) | |Drugs in Japan Vol. 6, Pg. 120, 1982. |- |dog |LDLo |parenteral |5ug/kg (0.005mg/kg) |CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION) |Pharmacology: International Journal of Experimental and Clinical Pharmacology. Vol. 1, Pg. 189, 1968. |- |guinea pig |LDLo |intravenous |100ug/kg (0.1mg/kg) | |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |guinea pig |LDLo |subcutaneous |800ug/kg (0.8mg/kg) | |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |infant |TDLo |multiple routes |625ug/kg/I (0.625mg/kg) |CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
LUNGS, THORAX, OR RESPIRATION: CYANOSIS
KIDNEY, URETER, AND BLADDER |"CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)" Southern Medical Journal. Vol. 78, Pg. 874, 1985. |- |man |LDLo |subcutaneous |7ug/kg (0.007mg/kg) |BRAIN AND COVERINGS: OTHER DEGENERATIVE CHANGES
CARDIAC: OTHER CHANGES |Annals of Emergency Medicine. Vol. 28, Pg. 725, 1996. |- |man |TDLo |intramuscular |2ug/kg (0.002mg/kg) |VASCULAR: REGIONAL OR GENERAL ARTERIOLAR CONSTRICTION |American Journal of Emergency Medicine. Vol. 8, Pg. 46, 1990. |- |man |TDLo |intravenous |16ug/kg (0.016mg/kg) |BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"
CARDIAC: CHANGE IN RATE
VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION |American Journal of Emergency Medicine. Vol. 5, Pg. 64, 1987. |- |man |TDLo |intravenous |285ug/kg (0.285mg/kg) |CARDIAC: EKG CHANGES NOT DIAGNOSTIC OF ABOVE |American Journal of Emergency Medicine. Vol. 7, Pg. 485, 1989. |- |man |TDLo |intravenous |3mg/kg (3mg/kg) |VASCULAR: CONTRACTION (ISOLATED TISSUES) |American Journal of Emergency Medicine. Vol. 8, Pg. 46, 1990. |- |man |TDLo |oral |77mg/kg (77mg/kg) |BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"
BEHAVIORAL: EXCITEMENT
GASTROINTESTINAL: NAUSEA OR VOMITING |Annals of Emergency Medicine. Vol. 19, Pg. 671, 1990. |- |man |TDLo |subcutaneous |8571ng/kg/80M (0.008571mg/kg) |CARDIAC: CARDIOMYOPATHY INCLUDING INFARCTION |American Heart Journal. Vol. 111, Pg. 1193, 1986. |- |man |TDLo |subcutaneous |43ug/kg (0.043mg/kg) |CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
GASTROINTESTINAL: NAUSEA OR VOMITING
SKIN AND APPENDAGES (SKIN): SWEATING: OTHER |Annals of Emergency Medicine. Vol. 19, Pg. 680, 1990. |- |mouse |LD50 |intraperitoneal |4mg/kg (4mg/kg) |Journal of Pharmacology and Experimental Therapeutics. Vol. 90, Pg. 110, 1947. |- |mouse |LD50 |intravenous |217ug/kg (0.217mg/kg) |BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)
CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP
SKIN AND APPENDAGES (SKIN): HAIR: OTHER |Acta Pharmacologica et Toxicologica. Vol. 38, Pg. 474, 1976. |- |mouse |LD50 |subcutaneous |1470ug/kg (1.47mg/kg) |Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. Vol. 202, Pg. 658, 1943. |- |mouse |LDLo |oral |50mg/kg (50mg/kg) |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |mouse |LDLo |unreported |10mg/kg (10mg/kg) |BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
LUNGS, THORAX, OR RESPIRATION: DYSPNEA
BEHAVIORAL: EXCITEMENT |Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. Vol. 162, Pg. 46, 1931. |- |rabbit |LD50 |intravenous |50ug/kg (0.05mg/kg) |LUNGS, THORAX, OR RESPIRATION: RESPIRATORY STIMULATION |Schweizerische Medizinische Wochenschrift. Vol. 71, Pg. 554, 1941. |- |rabbit |LD50 |subcutaneous |4mg/kg (4mg/kg) |LUNGS, THORAX, OR RESPIRATION: RESPIRATORY STIMULATION |Schweizerische Medizinische Wochenschrift. Vol. 71, Pg. 554, 1941. |- |rabbit |LDLo |oral |30mg/kg (30mg/kg) |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |rat |LD50 |intramuscular |3500mg/kg (3500mg/kg) |"Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973Vol. -, Pg. 105, 1973. |- |rat |LD50 |intravenous |150ug/kg (0.15mg/kg) |Archives Internationales de Pharmacodynamie et de Therapie. Vol. 41, Pg. 365, 1931. |- |rat |LD50 |skin |62mg/kg (62mg/kg) |BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)
BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
BEHAVIORAL: EXCITEMENT |Gigiena Truda i Professional'nye Zabolevaniya. Labor Hygiene and Occupational Diseases. Vol. 8(4), Pg. 30, 1964. |- |rat |LD50 |subcutaneous |5mg/kg (5mg/kg) |LUNGS, THORAX, OR RESPIRATION: RESPIRATORY STIMULATION |Schweizerische Medizinische Wochenschrift. Vol. 71, Pg. 554, 1941. |- |rat |LDLo |intraperitoneal |10mg/kg (10mg/kg) |BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD
BEHAVIORAL: MUSCLE WEAKNESS
LUNGS, THORAX, OR RESPIRATION: DYSPNEA |Journal of Pharmacology and Experimental Therapeutics. Vol. 88, Pg. 268, 1946. |- |rat |LDLo |oral |30mg/kg (30mg/kg) |"Structure et Activite Pharmacodyanmique des Medicaments du Systeme Nerveux Vegetatif," Bovet, D., and F. Bovet-Nitti, New York, S. Karger, 1948Vol. -, Pg. 22, 1948. |- |women |TDLo |intravenous |6ug/kg (0.006mg/kg) |CARDIAC: ARRHYTHMIAS (INCLUDING CHANGES IN CONDUCTION) |British Medical Journal. Vol. 286, Pg. 519, 1983. |- |}
