Labeled d8 Desmethyl Clozapine Hydrochloride Property

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Labeled d8 Desmethyl Clozapine Hydrochloride Chemical Properties,Usage,Production

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

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.Kuoppam?ki, M., Syv?lahti, 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)