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Cat. No.: HY-187004

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Norzotepine

Norzotepine is the major human metabolite of Zotepine (HY-103093) and also a NET inhibitor (human IC₅₀ = 4.2 nM). Norzotepine exerts antipsychotic-like and antidepressant-like effects by inhibiting Norepinephrine (HY-13715) reuptake and blocking dopamine D₂ (Dopamine D₂), histamine H₁ (Histamine H₁), and 5-HT₂ receptors. Norzotepine can be used for research on schizophrenia.

For research use only. We do not sell to patients.

CAS No.: 78846-91-0
Formula: C₁₇H₁₆ClNOS
Molecular Weight:317.83

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Norzotepine Chemical Structure

CAS No.: 78846-91-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

IC₅₀ & Target

^[2]^[4]

NET

4.2 nM (IC₅₀)

Dopamine D2 receptor

H₁ Receptor

5-HT₂ Receptor

All Dopamine Receptor Isoforms :

All Histamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	11 nM	Inhibition of norepinephrine reuptake in HEK293 cells transiently expressing mouse NET incubated with 100 nM [³H]NE for 30 mins. Inhibition of norepinephrine reuptake in HEK293 cells transiently expressing mouse NET incubated with 100 nM [³H]NE for 30 mins.	20223878
HEK293	IC50	4.2 nM	Inhibition of norepinephrine reuptake in HEK293 cells transiently expressing human NET incubated with 100 nM [³H]NE for 30 mins. Inhibition of norepinephrine reuptake in HEK293 cells transiently expressing human NET incubated with 100 nM [³H]NE for 30 mins.	20223878
HEK293	IC50	6191 nM	Inhibition of serotonin reuptake in HEK293 cells transiently expressing mouse SERT incubated with 50 nM [³H]5-HT for 30 mins. Inhibition of serotonin reuptake in HEK293 cells transiently expressing mouse SERT incubated with 50 nM [³H]5-HT for 30 mins.	20223878
CHO	IC50	38 nM	Antagonistic activity against human H1 receptor in CHO cells stably expressing H1 receptors stimulated with 1000 nM histamine measured by calcium flux assay using Fluo-4AM. Antagonistic activity against human H1 receptor in CHO cells stably expressing H1 receptors stimulated with 1000 nM histamine measured by calcium flux assay using Fluo-4AM.	20223878

In Vitro

Norzotepine (norZTP) (30 min) potently inhibits mouse and human NET with IC₅₀ values of 11 nM and 4.2 nM, respectively, while showing weak inhibition of mouse SERT with an IC₅₀ of 6191 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	C_max
Mice^[2]	3.2 mg/kg	i.p.	639 ng/g

In Vivo

Norzotepine (norZTP) (1-3 mg/kg; intraperitoneal injection) exerts antidepressant-like effects in the forced swim test, significantly reducing immobility time at 1 and 3 mg/kg intraperitoneal injection^[2].
Norzotepine (0.3-10 mg/kg; intraperitoneal injection) significantly inhibited MAP-induced hyperactivity, with an ED₅₀ of 0.33 mg/kg intraperitoneal injection^[2].
Norzotepine (1-10 mg/kg; intraperitoneal injection) does not induce catalepsy at doses up to 10 mg/kg, with an ED₅₀ of > 10 mg/kg^[2].
Norzotepine (1-10 mg/kg; intraperitoneal injection) inhibited APO-induced climbing with an ED₅₀ of 3.9 mg/kg and significantly induced biting at 3 mg/kg^[2].
Norzotepine (0.1-1 mg/kg; intraperitoneal injection) significantly antagonized Reserpine (HY-N0480)-induced hypothermia, with an intraperitoneal ED₅₀ of 0.23 mg/kg^[2].
Norzotepine (1-10 mg/kg; intraperitoneal injection) significantly reduced spontaneous locomotor activity at doses of 3 and 10 mg/kg, with an ED₅₀ of 3.1 mg/kg^[2].
Norzotepine (13.75 mg/kg; intraperitoneal injection; daily; 28 days) produced region-selective increases in D₁, D₂, and D₄ receptors and 5-HT_1A receptors, along with a decrease in 5-HT_2A receptors^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

DBA/2N (male, 13-14 weeks old)^[2]
Dosage:

1, 3 mg/kg
Administration:

i.p.; 30 min before testing
Result:

Significantly reduced immobility time at 1 and 3 mg/kg.

Animal Model:

ICR (male, 4-5 weeks old)^[2]
Dosage:

0.3, 1, 3, 10 mg/kg
Administration:

i.p.; 30 min before MAP injection
Result:

Significantly inhibited MAP-induced hyperlocomotion at 1, 3, and 10 mg/kg i.p. with an ED₅₀ of 0.33 mg/kg.

Animal Model:

ICR (male, 5 weeks old)^[2]
Dosage:

1, 3, 10 mg/kg
Administration:

i.p.; measured 30 min after injection
Result:

Did not induce catalepsy at 1, 3, and 10 mg/kg i.p. with a catalepsy-inducing ED₅₀ of > 10 mg/kg.
Incidence of catalepsy was 0% at 1, 3, and 10 mg/kg.

Animal Model:

ICR (male, 4 weeks old)^[2]
Dosage:

1, 3, 10 mg/kg (climbing); 3 mg/kg (gnawing)
Administration:

i.p.; 20 min before APO injection
Result:

Dose-dependently inhibited climbing behavior with significant reduction at 10 mg/kg i.p. and an ED₅₀ of 3.9 mg/kg.

Animal Model:

ICR (male, 7-8 weeks old)^[2]
Dosage:

0.1, 0.3, 1 mg/kg
Administration:

i.p.; 4 h after reserpine treatment
Result:

Dose-dependently inhibited hypothermia with an ED₅₀ of 0.23 mg/kg.
Showed 58% inhibition at 0.3 mg/kg.
Statistically significant change at 1 mg/kg.

Animal Model:

ICR (male, 4-5 weeks old)^[2]
Dosage:

1, 3, 10 mg/kg
Administration:

i.p.; 30 min before testing
Result:

Significantly reduced spontaneous locomotor activity at 3 and 10 mg/kg i.p. with an ED₅₀ of 3.1 mg/kg.

Animal Model:

Sprague-Dawley (Male, 200-225 g)^[4]
Dosage:

13.75 mg/kg
Administration:

i.p.; daily; 28 days
Result:

Increased D₁ receptor levels in nucleus accumbens by 28%, medial caudate putamen by 31%, and lateral caudate putamen by 32%.
Increased D₂ receptors in medial prefrontal cortex by 41%, nucleus accumbens by 40%, and hippocampus by 34%.
Increased D₄ receptors in nucleus accumbens by 78%, medial caudate putamen by 66%, and lateral caudate putamen by 52%.
Increased 5-HT₁A receptors in medial prefrontal cortex by 37% and dorsolateral frontal cortex by 41%.
Decreased 5-HT₂A receptors in medial prefrontal cortex by 44% and dorsolateral frontal cortex by 47%.

Chemical Information

CAS No. 78846-91-0
Molecular Weight 317.83
Formula C₁₇H₁₆ClNOS
SMILES

ClC=1C=CC=2SC=3C=CC=CC3C=C(OCCNC)C2C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Marcus MM, et al. Augmentation by escitalopram, but not citalopram or R-citalopram, of the effects of low-dose risperidone: behavioral, biochemical, and electrophysiological evidence. Synapse (New York, N.Y.). 2012 Apr;66(4):277-90.

[2]. Shobo M, et al. Norzotepine, a major metabolite of zotepine, exerts atypical antipsychotic-like and antidepressant-like actions through its potent inhibition of norepinephrine reuptake. The Journal of pharmacology and experimental therapeutics. 2010 Jun;333(3):772-81.

[3]. Barnas C, et al. In vivo (123)I IBZM SPECT imaging of striatal dopamine 2 receptor occupancy in schizophrenic patients. Psychopharmacology. 2001 Sep;157(3):236-42.

[4]. Liégeois JF, et al. New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. Journal of medicinal chemistry. 2012 Feb 23;55(4):1572-82.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Norzotepine

All Dopamine Receptor Isoforms

All Histamine Receptor Isoforms

All 5-HT Receptor Isoforms