APOMORPHINE HYDROCHLORIDE
- CAS No.
- 314-19-2
- Chemical Name:
- APOMORPHINE HYDROCHLORIDE
- Synonyms
- (r)-id;UPRIMA;TAK251);KW-6500;R(–)-APO;NSC 11442;APL130277;(theta)-id;APL 130277;APL-130277
- CBNumber:
- CB8357092
- Molecular Formula:
- C17H18ClNO2
- Molecular Weight:
- 303.78
- MOL File:
- 314-19-2.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/6/30 15:45:59
| Melting point | >250℃ |
|---|---|
| storage temp. | Store at RT |
| solubility | ≥1.08 mg/mL in EtOH with ultrasonic; ≥12.9 mg/mL in DMSO; ≥5.12 mg/mL in H2O |
| form | solid |
| EPA Substance Registry System | Apomorphine hydrochloride (314-19-2) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H334-H312-H332-H317 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501-P261-P271-P304+P340-P312-P280-P302+P352-P312-P322-P363-P501-P261-P272-P280-P302+P352-P333+P313-P321-P363-P501-P261-P285-P304+P341-P342+P311-P501 | |||||||||
| RIDADR | 3249 | |||||||||
| HazardClass | 6.1(b) | |||||||||
| PackingGroup | III | |||||||||
| Toxicity | mmo-sat 20 mg/plate MUREAV 137,17,84 | |||||||||
| NFPA 704 |
|
APOMORPHINE HYDROCHLORIDE Chemical Properties,Uses,Production
Uses
Emetic.
General Description
Apomorphine hydrochloride,(6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolone-10,11-diol hydrochloride (Apokyn), is awhite or off-white powder or crystal soluble in hot water(pKa＝8.92). Apormorphine is an aporphine alkaloid of thebenzoquinoline class. Oral apomorphine is poorly absorbedand has a bioavailability of less than 4%. Upon subcutaneousadministration, apomorphine is completely absorbed. Within10 to 20 minutes, the maximum concentration of the drug isdistributed from the blood plasma to the CSF. Other potentialroutes of administration include continuous subcutaneous infusion,intravenous infusion, intranasal spray application,sublingual, and rectal administration.23 The agent is highlylipophilic in nature, allowing for rapid diffusion across theBBB after injection. Apomorphine has a short plasma halflife;however, clinical effects may last from 60 to 90 minutes.Apomorphine displays a significant degree of interpatientvariability in its pharmacokinetic profile. Studies of bothintravenous and subcutaneous injection routes found this variation was not attributable to body weight, age, gender,and duration of PD or L-DOPA dose/duration alone.Apomorphine is extensively metabolized. Hypothesizedroutes include sulfation, N-demethylation, glucuronidation,and oxidation. Subcutaneous injections of apomorphine arerenally and hepatically cleared, with the majority appearingto be renally cleared. Dosage adjustments are needed in bothliver and renal impairment. The activity of apomorphine isbelieved to be caused by stimulation of postsynaptic D1- andD2-type receptors within the caudate/putamen in the brain.Apomorphine is indicated for the acute, intermittent treatmentof hypomobility, “off” episodes (“end-of-dose wearingoff” and unpredictable on/off episodes) associated with advancedPD.
Biological Activity
Prototypical dopamine agonist (pK i values are 6.43, 7.08, 7.59, 8.36 and 7.83 for human recombinant D 1 , D 2L , D 3 , D 4 and D 5 receptors respectively). Produces biphasic effects on locomotor activity, and displays anti-Parkinsonian and neuroprotective actions following systemic administration in vivo .
Safety Profile
Poison by intravenous andintraperitoneal routes. Mutation data reported. When heated to decomposition itemits very toxic fumes of NOx and HCl.
APOMORPHINE HYDROCHLORIDE Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Rusan Pharma Ltd | +91-2228687035 +91-9690022465 | Maharashtra, India | 14 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Euroasia Trans Continental | +91 22 56349035-36 | New Delhi, India | 519 | 47 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| Shaanxi Dideu Medichem Co. Ltd | +86-029-89586680 +86-18192503167 | China | 9030 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | China | 20314 | 58 | Inquiry |
| InvivoChem | 13549236410 | China | 6749 | 58 | Inquiry |
| Cayman Chemical Company | (800) 364-9897 | United States | 6618 | 81 | Inquiry |
| MP Biomedicals, Inc. | 949 833 2500 | United States | 6566 | 81 | Inquiry |
| Supplier | Advantage |
|---|---|
| Rusan Pharma Ltd | 58 |
| CLEARSYNTH LABS LTD. | 58 |
| Euroasia Trans Continental | 47 |
| TargetMol Chemicals Inc. | 58 |
| Shaanxi Dideu Medichem Co. Ltd | 58 |
| InvivoChem | 58 |
| Henan Fengda Chemical Co., Ltd | 58 |
| InvivoChem | 58 |
| Cayman Chemical Company | 81 |
| MP Biomedicals, Inc. | 81 |
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