PRODUCT INFORMATION
Names
| Name | L-α-Methyl DOPA Hydrate |
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| Synonym | More Synonyms |
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Methyldopa Sesquihydrate Biological Activity
| Description | L-(-)-α-Methyldopa hydrate is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.Target: alpha-adrenergic agonistMethyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. Its use is now mostly deprecated following the introduction of alternative safer classes of agents. However, it continues to have a role in otherwise difficult to treat hypertension and gestational hypertension (also known as pregnancy-induced hypertension (PIH)).Methyldopa has a dual mechanism of action. It is a competitive inhibitor of the enzyme DOPA decarboxylase, also known as aromatic L-amino acid decarboxylase, which converts L-DOPA into dopamine. Dopamine is a precursor for norepinephrine (noradrenaline) and subsequently epinephrine (adrenaline). This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. This effect may lower blood pressure and cause central nervous system effects such as depression, anxiety, apathy, anhedonia, and parkinsonism. It is converted to α-methylnorepinephrine by dopamine beta-hydroxylase (DBH). α-methylnorepinephrine is an agonist of presynaptic central nervous system α2-adrenergic receptors. Activation of these receptors in the brainstem appears to inhibit sympathetic nervous system output and lower blood pressure. This is also the mechanism of action of clonidine. |
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| Related Catalog | Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Cardiovascular Disease |
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| References | [1]. BAILA MR, et al. The use of the combination of L-alpha-methyldopa and dichlorothiazide in the treatment of arterial hypertension. Dia Med. 1962 Dec 6;34:2422-4. |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 441.6±45.0 °C at 760 mmHg |
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| Melting Point | >300 °C(lit.) |
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| Molecular Formula | C10H13NO4.3/2H2O |
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| Molecular Weight | 238.24 |
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| Flash Point | 220.9±28.7 °C |
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| PSA | 113.01000 |
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| LogP | 0.13 |
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| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
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| Index of Refraction | 1.635 |
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| Storage condition | Refrigerator |
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| Stability | Stable, but may be light sensitive. Very hygroscopic. Undergoes catalytic oxygenation in the presence of magnesium, cupric, cobalt, nickel and ferric ions. Store under a dry atmosphere. |
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| Water Solubility | 0.1-1 g/100 mL at 23 ºC |
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MSDS
Methyldopa Sesquihydrate MSDS(Chinese) |
Toxicological Information
CHEMICAL IDENTIFICATIONCAS REGISTRY NUMBER : 41372-08-1
MOLECULAR FORMULA : C10-H13-N-O4.3/2H2-O
HEALTH HAZARD DATAACUTE TOXICITY DATASPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 17500 mg/kg/14D-C
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 68250 mg/kg/13W-C
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 604 gm/kg/2Y-C
TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - other effects on male Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)
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Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| Risk Phrases | R20/21:Harmful by inhalation and in contact with skin . R36/37/38:Irritating to eyes, respiratory system and skin . R42/43:May cause sensitization by inhalation and skin contact . R65:Harmful: May cause lung damage if swallowed. |
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| Safety Phrases | S24/25 |
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| RIDADR | NONH for all modes of transport |
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| WGK Germany | 3 |
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| RTECS | YP2860000 |
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