| Company Name: |
Energy Chemical |
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400-0056266 |
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marketing1@energy-chemical.com |
Labeled d8 Desmethyl Clozapine Hydrochloride manufacturers
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| | Labeled d8 Desmethyl Clozapine Hydrochloride Basic information |
| Product Name: | Labeled d8 Desmethyl Clozapine Hydrochloride | | Synonyms: | Labeled d8 Desmethyl Clozapine Hydrochloride;N-DESMETHYLCLOZAPINE (D8, 98%) 100 UG/ML IN METHANOL;[2H8]-N-Desmethyl Clozapine;6-chloro-10-[(2,2,3,3,5,5,6,6-2H?)piperazin-1-yl]-2,9-diazatricyclo[9.4.0.03,?]pentadeca-1(11),3(8),4,6,9,12,14-heptaene;N-Desmethylclozapine-D8 solution;D8-N-Desmethyl Clozapine | | CAS: | 1189888-77-4 | | MF: | C17H17ClN4 | | MW: | 312.8 | | EINECS: | | | Product Categories: | | | Mol File: | 1189888-77-4.mol |  |
| | Labeled d8 Desmethyl Clozapine Hydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml | | form | A solid | | color | White to off-white | | Major Application | clinical testing |
| WGK Germany | WGK 2 | | Storage Class | 3 - Flammable liquids | | Hazard Classifications | Acute Tox. 3 Dermal
Acute Tox. 3 Inhalation
Acute Tox. 3 Oral
Flam. Liq. 2
STOT SE 1 |
| | Labeled d8 Desmethyl Clozapine Hydrochloride Usage And Synthesis |
| Uses | A major labelled metabolite of clozapine. A potent and selective 5-HT2C serotonin receptor antogonist. | | Biological Activity | N-Desmethylclozapine-d8 is intended for use as an internal standard for the quantification of N-desmethylclozapine by GC- or LC-MS. N-Desmethylclozapine is an active metabolite of the atypical antipsychotic clozapine .1 It was originally described as an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50 = 7.1 nM in rat choroid plexus) and later as an inverse agonist using human recombinant receptors.2,3 N-Desmethylclozapine is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors, and a partial agonist at dopamine D2 and D3, M1 muscarinic acetylcholine, and 5-HT1A receptors.3,1,4 N-Desmethylclozapine (30 mg/kg) decreases exploratory locomotor activity and increases prepulse inhibiton of the acoustic startle response in mice.5 | | IC 50 | mAChR1; δ Opioid Receptor/DOR | | References | 1.Burstein, E.S., Ma, J., Wong, S., et al.Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonistJ. Pharmacol. Exp. Ther.315(3)1278-1287(2005)
2.Kuoppamki, M., Syvlahti, E., and Hietala, J.Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonistsEur. J. Pharmacol.245(2)179-182(1993)
3.Lameh, J., Burstein, E.S., Taylor, E., et al.Pharmacology of N-desmethylclozapinePharmacol. Ther.115(2)223-231(2007)
4.Odagaki, Y., Kinoshita, M., and Ota, T.Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranesJ. Psychopharmacol.30(9)896-912(2016)
5.Maehara, S., Hikichi, H., and Ohta, H.Behavioral effects of N-desmethylclozapine on locomotor activity and sensorimotor gating function in mice-Possible involvement of muscarinic receptorsBrain Res.1418111-119(2011) |
| | Labeled d8 Desmethyl Clozapine Hydrochloride Preparation Products And Raw materials |
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