An atypical antipsychotic
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Clozapine (hydrochloride)

Item No. 25779

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine, dihydrochloride
CAS Number
2711603-38-0
Molecular Formula
C18H19ClN4 • 2HCl
Formula Weight
399.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
213, 228, 259 nm
SMILES
ClC(C=C1)=CC2=C1NC(C=CC=C3)=C3C(N4CCN(C)CC4)=N2.Cl.Cl
InChi Code
InChI=1S/C18H19ClN4.2ClH/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18;;/h2-7,12,20H,8-11H2,1H3;2*1H
InChi Key
FBIKVTKYNDDABY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

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    Product Description

    Clozapine is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 180 nM).1,2 It also binds to the 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 receptors (Kis = 3.3, 13, 110, 4, and 21 nM, respectively), as well as the histamine H1 and α1-adrenergic receptors (Kis = 2.1 and 23 nM, respectively). It does not bind to the 5-HT1B receptor and has a lower affinity for dopamine receptors (Kis = 540, 150, and 360 nM for D1-3, respectively). Clozapine induces the release of glutamate and D-serine, an agonist at the glycine site of the NMDA receptor, from astrocytes, and reduces the expression of astrocytic glutamate transporters.3 It reverses locomotor hyperactivity and deficits in prepulse inhibition of acoustic startle in a rat neonatal ventral hippocampal ibotenic lesion model of schizophrenia when administered at a dose of 2.5 mg/kg per day.4 Formulations containing clozapine have been used in the treatment of schizophrenia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Millan, M.J. Improving the treatment of Schizophrenia: Focus on serotonin (5-HT)1A receptors. J. Pharmacol. Exp. Ther. 295(3), 853-861 (2000).

    2. Schotte, A., Janssen, P.F., Gommeren, W., et al. Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding. Psychopharmacology (Berl) 124(1-2), 57-73 (1996).

    3. Tanahashi, S., Yamamura, S., Nakagawa, M., et al. Clozapine, but not haloperidol, enhances glial ᴅ-serin and L-glutamate release in rat frontal cortex and primary cultured astrocytes. Br. J. Pharmacol. 165(5), 1543-1555 (2012).

    4. Rueter, L.E., Ballard, M.E., Gallagher, K.B., et al. Chronic low dose risperidone and clozapine alleviate positive but not negative symptoms in the rat neonatal ventral hippocampal lesion model of schizophrenia. Psychopharmacology (Berl.) 176(3-4), 312-319 (2004).