Pilocarpine Hydrochloride structure
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Common Name | Pilocarpine Hydrochloride | ||
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CAS Number | 54-71-7 | Molecular Weight | 208.257 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 431.8±18.0 °C at 760 mmHg | |
Molecular Formula | C11H17ClN2O2 | Melting Point | 202-205 °C(lit.) | |
MSDS | Chinese USA | Flash Point | 215.0±21.2 °C | |
Symbol |
GHS06 |
Signal Word | Danger |
Use of Pilocarpine HydrochloridePilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist. |
Name | (+)-Pilocarpine hydrochloride |
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Synonym | More Synonyms |
Description | Pilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist. |
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Related Catalog | |
Target |
M3 muscarinic receptor[1] |
In Vitro | To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls[2]. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM)[3]. |
In Vivo | The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na+ concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05)[1]. |
Cell Assay | Cell viability is determined by MTT assay. Briefly, HCS cells are inoculated into a 96-well culture plate (Nunc) at a density of 1×104 cells/100 µL/well, and are cultured and treated. At a 4h interval, the Pilocarpine (0.625 to 20 g/L)-containing medium is replaced entirely with 100 µL serum-free DMEM/F12 medium containing 1.0 g/L MTT, and the cells are incubated at 37°C in the dark for 4h. After the MTT-containing medium is discarded with caution, 150 µL DMSO is added to dissolve the produced formazan crystals at 37°C in the dark for 15 min, and the absorbance at 490 nm is measured with a Multiskan GO microplate reader[2]. |
Animal Admin | Rats[1] Male, 10-week-old Wistar rats are assigned to one of two groups, exercise (EX, n=6) and control (CN, n=6). The EX rats are kept for 40 days in cages with a running wheel (SN-451), allowing them to undertake voluntary exercise, while the CN rats are kept in cages with the running wheel locked. On the 40th day, Pilocarpine-induced saliva is measured as follows. Briefly, the rats are anesthetized, preweighed cotton was placed in their mouths sublingually, and Pilocarpine (0.5 mg/kg) is intraperitoneally injected to induce saliva secretion. Each cotton ball is then changed every 10 min for 1 h. The collected cotton balls are weighed again, and the mass of saliva secreted is calculated by subtracting the initial from the final weight. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 431.8±18.0 °C at 760 mmHg |
Melting Point | 202-205 °C(lit.) |
Molecular Formula | C11H17ClN2O2 |
Molecular Weight | 208.257 |
Flash Point | 215.0±21.2 °C |
Exact Mass | 208.121185 |
PSA | 44.12000 |
LogP | -0.09 |
Vapour Pressure | 0.0±1.0 mmHg at 25°C |
Index of Refraction | 1.585 |
Water Solubility | soluble |
Synonym:Almocarpine; Pilocar; Pilomiotin Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
Risk Phrases: 26/28 Section 3 - HAZARDS IDENTIFICATION EMERGENCY OVERVIEW
Very toxic by inhalation and if swallowed.Hygroscopic (absorbs moisture from the air).The toxicological properties of this material have not been fully investigated. Potential Health Effects Eye: May cause eye irritation. Skin: May cause skin irritation. May be harmful if absorbed through the skin. Ingestion: May cause irritation of the digestive tract. The toxicological properties of this substance have not been fully investigated. May be harmful if swallowed. Inhalation: May be fatal if inhaled. May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated. Chronic: No information found. Section 4 - FIRST AID MEASURES Eyes: Immediately flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid immediately. Skin: Get medical aid immediately. Immediately flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Ingestion: Never give anything by mouth to an unconscious person. SPEED IS ESSENTIAL. A DOCTOR MUST BE NOTIFIED AT ONCE. Do NOT induce vomiting. If conscious and alert, rinse mouth and drink 2-4 cupfuls of milk or water. Wash mouth out with water. Inhalation: Get medical aid immediately. Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Notes to Physician: Treat symptomatically and supportively. Section 5 - FIRE FIGHTING MEASURES General Information: As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. This material in sufficient quantity and reduced particle size is capable of creating a dust explosion. Extinguishing Media: Use water spray, dry chemical, carbon dioxide, or chemical foam. Use agent most appropriate to extinguish fire. Section 6 - ACCIDENTAL RELEASE MEASURES General Information: Use proper personal protective equipment as indicated in Section 8. Spills/Leaks: Clean up spills immediately, observing precautions in the Protective Equipment section. Sweep up, then place into a suitable container for disposal. Avoid generating dusty conditions. Provide ventilation. Section 7 - HANDLING and STORAGE Handling: Wash thoroughly after handling. Minimize dust generation and accumulation. Do not breathe dust, vapor, mist, or gas. Do not get in eyes, on skin, or on clothing. Keep container tightly closed. Use only in a chemical fume hood. Storage: Store in a cool, dry place. Store in a tightly closed container. Store protected from moisture. Store protected from light. Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION Engineering Controls: Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low. Exposure Limits CAS# 54-71-7: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166. Skin: Wear appropriate protective gloves to prevent skin exposure. Clothing: Wear appropriate protective clothing to prevent skin exposure. Respirators: Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Use a NIOSH/MSHA or European Standard EN 149 approved respirator if exposure limits are exceeded or if irritation or other symptoms are experienced. Section 9 - PHYSICAL AND CHEMICAL PROPERTIES Physical State: Crystalline powder Color: white to off-white Odor: odorless pH: 3.5 - 4.5 (5%aq.sol) Vapor Pressure: Not available. Viscosity: Not available. Boiling Point: Not available. Freezing/Melting Point: 200-204 deg C Autoignition Temperature: Not available. Flash Point: Not available. Explosion Limits, lower: Not available. Explosion Limits, upper: Not available. Decomposition Temperature: Solubility in water: Freely Soluble. Specific Gravity/Density: Molecular Formula: C11H16N2O2.HCl Molecular Weight: 244.72 Section 10 - STABILITY AND REACTIVITY Chemical Stability: Stable. Conditions to Avoid: Incompatible materials, light, dust generation, excess heat, exposure to moist air or water. Incompatibilities with Other Materials: Moisture, oxidizing agents. Hazardous Decomposition Products: Hydrogen chloride, nitrogen oxides, carbon monoxide, irritating and toxic fumes and gases, carbon dioxide, oxides of chlorine. Hazardous Polymerization: Will not occur. Section 11 - TOXICOLOGICAL INFORMATION RTECS#: CAS# 54-71-7: TK1450000 LD50/LC50: CAS# 54-71-7: Oral, mouse: LD50 = 200 mg/kg. Carcinogenicity: (+)-Pilocarpine Hydrochloride - Not listed by ACGIH, IARC, or NTP. Other: See actual entry in RTECS for complete information. Section 12 - ECOLOGICAL INFORMATION Section 13 - DISPOSAL CONSIDERATIONS Dispose of in a manner consistent with federal, state, and local regulations. Section 14 - TRANSPORT INFORMATION IATA Shipping Name: TOXIC SOLID, ORGANIC, N.O.S.* Hazard Class: 6.1 UN Number: 2811 Packing Group: III IMO Shipping Name: TOXIC SOLID, ORGANIC, N.O.S. Hazard Class: 6.1 UN Number: 2811 Packing Group: III RID/ADR Shipping Name: TOXIC SOLID, ORGANIC, N.O.S. Hazard Class: 6.1 UN Number: 2811 Packing group: III Section 15 - REGULATORY INFORMATION European/International Regulations European Labeling in Accordance with EC Directives Hazard Symbols: T+ Risk Phrases: R 26/28 Very toxic by inhalation and if swallowed. Safety Phrases: S 25 Avoid contact with eyes. S 45 In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible). WGK (Water Danger/Protection) CAS# 54-71-7: 3 Canada CAS# 54-71-7 is listed on Canada's NDSL List. CAS# 54-71-7 is not listed on Canada's Ingredient Disclosure List. US FEDERAL TSCA CAS# 54-71-7 is listed on the TSCA inventory. SECTION 16 - ADDITIONAL INFORMATION N/A |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
Symbol |
GHS06 |
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Signal Word | Danger |
Hazard Statements | H300 + H330 |
Precautionary Statements | Missing Phrase - N15.00950417-P260-P304 + P340 + P310-P403 + P233 |
Hazard Codes | T+:Verytoxic; |
Risk Phrases | R26/28 |
Safety Phrases | S25-S45 |
RIDADR | UN 1544 6.1/PG 3 |
WGK Germany | 3 |
RTECS | TK1450000 |
Packaging Group | III |
Hazard Class | 6.1 |
HS Code | 2934999090 |
~% Pilocarpine Hyd... CAS#:54-71-7 |
Literature: Tetrahedron, , vol. 65, # 39 p. 8283 - 8296 |
HS Code | 2934999090 |
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Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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(3S,4R) |
pilocel |
Akarpine |
Pilocarpine HCl |
2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, (3S-cis)- |
pilocarpine,2(3H)-furanone,3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)-methyl] monohydrochloride,(3S-cis) |
Salagen |
Pilocarpine |
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)-methyl]dihydrofuran-2(3H)one hydrochloride |
pilovisc |
EINECS 200-212-5 |
Sanpilo |
2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, (3S,4R)- |
Pilocarpine (Hydrochloride) |
(3S,4R)-3-Ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydro-2(3H)-furanone |
MFCD00012722 |
pilocar |
ami-pilo |
(+)-pilocarpine |
(3S,4R)-3-Ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one |
amisturap |
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, (3S-cis)- |