Adrenergic Receptor
α-adrenoceptor [1][2]
β-adrenoceptor (β1, β2 subtypes) [1][2]

In vitro activity: Epinephrine is a hormone and a neurotransmitter. The study of the pharmacology of adrenaline has significantly advanced our knowledge of the autonomic nervous system and the role of the sympathetic nervous system. For a number of emergency situations, epinephrine is still a helpful medication. This is true even though it acts non-specifically on adrenoceptors and several selective medications targeting different adrenoceptor subtypes have since been developed. Although this is physiologically incorrect, the term "adrenaline" is commonly used to refer to increased sympathetic system activation linked to the vigor and excitement of the fight-or-flight response. Adrenaline primarily affects organs without direct sympathetic innervation through its effects on metabolism and bronchodilation.

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DL-Adrenaline induced concentration-dependent contraction of isolated rabbit aortic smooth muscle. Treatment with 0.01-1 μM for 15 minutes caused a maximal contraction amplitude of ~80% compared to KCl-induced contraction, mediated via α-adrenoceptor activation [1]
It produced concentration-dependent relaxation of histamine-precontracted human isolated bronchial smooth muscle. At concentrations of 0.1-10 μM, it relaxed smooth muscle by ~30-90%, with an EC50 of 0.8 μM, via β2-adrenoceptor stimulation [2]

In anesthetized dogs, intravenous administration of DL-Adrenaline (0.1-1 mg/kg) dose-dependently increased systolic blood pressure. At 1 mg/kg, systolic blood pressure rose by ~40% within 5 minutes, accompanied by a transient increase in heart rate (~25%) [1]
In patients with bronchial asthma, subcutaneous injection of DL-Adrenaline (0.3 mg) significantly reduced airway resistance by ~35% within 15 minutes and improved forced expiratory volume in 1 second (FEV1) by ~28% compared to baseline, lasting for ~1 hour [2]

Anesthetized dog hemodynamic assay: Adult dogs are anesthetized with sodium pentobarbital, and a femoral artery catheter is implanted to monitor blood pressure. A jugular vein catheter is placed for drug administration. DL-Adrenaline is dissolved in physiological saline and administered intravenously at doses of 0.1, 0.5, or 1 mg/kg. Systolic/diastolic blood pressure and heart rate are recorded at baseline, 1, 5, 10, 20, and 30 minutes post-administration [1]

Absorption, Distribution and Excretion
For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668]. Absorption, Distribution and Excretion
For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668]. Absorption, Distribution and Excretion
For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668]. Absorption, Distribution and Excretion
For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668]. Absorption, Distribution and Excretion
For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668]. [DB00668].

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Absorption: After subcutaneous injection of DL-adrenaline, it is rapidly absorbed by the human body, and the peak plasma concentration is reached within 15-30 minutes [2].
Metabolism: DL-adrenaline is rapidly metabolized in the liver and tissues by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO) to generate inactive metabolites [2].
Elimination: The plasma elimination half-life of DL-adrenaline in the human body is about 2-3 minutes, and about 80% of the dose is excreted in the urine as metabolites within 24 hours [2].

Effects During Pregnancy and Lactation
◉ Overview of Drug Use During Lactation
There is currently no information regarding the use of epinephrine during lactation. Due to its low oral bioavailability and short half-life, epinephrine in breast milk is unlikely to affect the infant. High-dose intravenous epinephrine may reduce milk production or the milk ejection reflex. Low-dose intramuscular injections (e.g., Epi-Pen), epidural injections, topical application, inhalation, or ophthalmic epinephrine are unlikely to interfere with breastfeeding. After using eye drops, to significantly reduce the effect of the medication, press the tear duct at the corner of the eye for at least 1 minute, then wipe away any excess medication with absorbent tissue. Epinephrine is the first-line drug for treating anaphylactic shock; it should be used in the same manner in both lactating and non-lactating patients.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
As of the revision date, no published information was found regarding lactating mothers. In non-lactating subjects and women with hyperprolactinemia, intravenous epinephrine infusion decreased serum prolactin concentrations. Animal data indicated that intra-arterial epinephrine injection decreased serum oxytocin levels and inhibited milk production. However, low-dose epinephrine infusion as part of epidural analgesia did not impair breastfeeding in lactating mothers. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed.
An Egyptian study compared the effects of 2% lidocaine (n=75) and 2% lidocaine combined with 1:200,000 epinephrine (n=70) in wound infiltration anesthesia after cesarean section. Patients receiving lidocaine combined with epinephrine initiated breastfeeding 89 minutes post-surgery, while those receiving lidocaine alone required 132 minutes. The difference was statistically significant.

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Protein binding For pharmacokinetic data on levodopaminergic agonist, please refer to the drug entry for [DB00668].

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Common adverse reactions in humans include palpitations (occurring in approximately 20%), transient hypertension (approximately 15%), and tremor (approximately 10%). These adverse reactions are dose-related and resolve within 1–2 hours [2].
In anesthetized dogs, intravenous administration of doses ≥5 mg/kg resulted in ventricular arrhythmias and severe hypertension, with death observed at doses of 10 mg/kg [1].

[1]. Am J Physiol . 1982 Apr;242(4):H593-601.

[2]. Br J Dis Chest . 1986 Jan;80(1):1-6.

3,4-dihydroxyl-α-[methylamino]methylbenzyl alcohol is an odorless, light brown or nearly white crystal. (NTP, 1992)
Adrenaline is a racemic mixture composed of equimolar amounts of (R)-adrenaline and (S)-adrenaline. It is a human metabolite. It contains (R)-adrenaline and (S)-adrenaline.
The adrenaline ring is a racemic mixture of d-[DB00668] and l-[DB00668] enantiomers. Adrenaline is a non-selective α- and β-adrenergic receptor agonist. It is a bronchodilator used to temporarily relieve mild symptoms of intermittent asthma, including wheezing, chest tightness, and shortness of breath. It is the active ingredient in over-the-counter oral inhalers, existing as epinephrine hydrochloride.
L-adrenaline has been reported in the human body, and relevant data exist. It is a racemic mixture of dextro- and levo-adrenaline. See also: epinephrine hydrochloride (in salt form); epinephrine (note moved to). Drug Indications For temporary relief of mild symptoms of intermittent asthma. FDA Label Mechanism of Action Epinephrine is a nonselective agonist of α- and β-adrenergic receptors, both of which are G protein-coupled receptors. The primary therapeutic effect of epinephrine derives from its agonistic effect on β2-adrenergic receptors, which activates adenylate cyclase and increases intracellular production of cyclic adenosine monophosphate (cAMP). Epinephrine relaxes smooth muscle in various tissues, including bronchial smooth muscle. Therefore, epinephrine helps relieve bronchospasm, wheezing, and chest tightness that may occur during an asthma attack. Adrenaline, through its relaxing effect on the smooth muscles of the stomach, intestines, uterus, and bladder, can relieve itching, urticaria, and angioedema, and can alleviate gastrointestinal and genitourinary symptoms associated with allergic reactions. Adrenaline also acts on α-adrenergic receptors on vascular smooth muscle, particularly in the vascular beds of the skin and internal organs, causing vasoconstriction. Adrenaline is believed to reduce capillary leakage by constricting precapillary arterioles, thereby lowering hydrostatic pressure and reducing bronchial mucosal edema.

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DL-adrenaline is a non-selective adrenergic receptor agonist that activates α and β (β1, β2) subtypes[1][2]
Its mechanism of action includes α-adrenaline receptor-mediated vasoconstriction (increased blood pressure) and β2-adrenaline receptor-mediated smooth muscle relaxation (relief of bronchospasm)[1][2]
Based on its rapid bronchodilation, it is clinically applicable for the emergency treatment of acute bronchial asthma attacks[2]
It has dual hemodynamic and respiratory effects, making it a key drug for the treatment of life-threatening bronchospasm and hypotensive emergencies[1][2]

C9H13NO3

183.2

183.089

C, 59.00; H, 7.15; N, 7.65; O, 26.20

329-65-7

329-65-7; 329-63-5 (HCl)

838

Solid powder

1.3±0.1 g/cm3

413.1±40.0 °C at 760 mmHg

197 °C (dec.)(lit.)

207.9±17.9 °C

0.0±1.0 mmHg at 25°C

1.608

-0.63

4

4

3

13

154

0

OC(C1=CC(O)=C(O)C=C1)CNC

UCTWMZQNUQWSLP-UHFFFAOYSA-N

InChI=1S/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3

4-[1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)