1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. Molindone (hydrochloride)

Molindone (hydrochloride)  (Synonyms: EN-1733A)

Art. -Nr.: HY-B1017 Reinheit: 99.81%
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Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease.

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Molindone (hydrochloride)

Molindone (hydrochloride) Chemische Struktur

CAS. Nr. : 15622-65-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Beschreibung

Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease[1][2].

IC50 & Target[1]

D2 Receptor

 

D5 Receptor

 

In Vitro

Molindone hydrochloride scarcely affects rat brain MAO activity in vitro, with a IC50 of 9.8 × 10-3 M[2].

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

In Vivo

Molindone hydrochloride (5-60 mg/kg-bw/day; i.g.,; daily; 13 weeks) induces dose-dependent CNS effects, body weight and food consumption reductions in males, serum chemistry alterations, organ weight changes, transient prolactin surges, and mild histopathological changes in reproductive and hepatic tissues in adult Wistar Han rats[1].
Molindone hydrochloride (5-75 mg/kg-bw/day; i.g.; daily; 8 weeks) induces dose-dependent CNS effects, body weight and food consumption reductions in males, serum chemistry alterations, organ weight changes, and delays in sexual maturation (attributed to reduced body weights), with most effects resolving during a 6-week non-dosing recovery period; no significant adverse effects on reproductive function are observed when administered orally to juvenile CD Sprague-Dawley rats[1].
Molindone hydrochloride (p.o.) exhibits neuroleptic and antidepressant activityin rats[2].
Molindone hydrochloride (1-2 mg/kg; p.o.) blocks Apomorphine (HY-12723)-induced emesis in dogs[2].
Molindone hydrochloride (0.5-1 mg/kg; p.o.) reduces aggressiveness for 2-3 hours, with higher doses producing gradual, sustained docility in Macaca mulatta[2].

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

Animal Model: GF1 mice (male)[2]
Dosage: 2.5 mg/kg (tetrabenazine-induced ptosis ED50); 10.0 mg/kg (5-HTP potentiation ED50); 12.0 mg/kg (DOPA potentiation ED50); 5-15 mg/kg (catalepsy, hypothermia)
Administration: p.o.; 1 hour before test assessment
Result: Suppressed spontaneous locomotion, blocked conditioned avoidance responses, and antagonized amphetamine-induced stereotyped behaviour; relative potency vs.
chlorpromazine was 0.23 (locomotor suppression), 0.17 (avoidance blockade), and 0.31 (amphetamine antagonism).
Achieved an ED50 of 2.5 mg/kg for antagonizing tetrabenazine-induced ptosis.
Achieved an ED50 of 10.0 mg/kg for potentiating 5-hydroxytryptophan (5-HTP) effects.
Achieved an ED50 of 12.0 mg/kg for potentiating 3,4-dihydroxyphenylalanine (DOPA) effects.
Induced catalepsy and hypothermia at oral doses of 5-15 mg/kg.
Animal Model: Rhesus monkey[2]
Dosage: 0.5, 1 mg/kg
Administration: p.o.
Result: Curtailed aggressiveness for 2-3 hours at oral doses of 0.5-1 mg/kg.
Increasing doses gradually increased the degree and duration of docility, with a more gradual response than chlorpromazine.
Molekulargewicht

312.83

Formel

C16H25ClN2O2

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(NC(C)=C2CC)CCC1CN3CCOCC3.[H]Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit
In Vitro: 

H2O : 100 mg/mL (319.66 mM; Need ultrasonic)

DMSO : 17.5 mg/mL (55.94 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1966 mL 15.9831 mL 31.9662 mL
5 mM 0.6393 mL 3.1966 mL 6.3932 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.1966 mL 15.9831 mL 31.9662 mL 79.9156 mL
5 mM 0.6393 mL 3.1966 mL 6.3932 mL 15.9831 mL
10 mM 0.3197 mL 1.5983 mL 3.1966 mL 7.9916 mL
15 mM 0.2131 mL 1.0655 mL 2.1311 mL 5.3277 mL
20 mM 0.1598 mL 0.7992 mL 1.5983 mL 3.9958 mL
25 mM 0.1279 mL 0.6393 mL 1.2786 mL 3.1966 mL
30 mM 0.1066 mL 0.5328 mL 1.0655 mL 2.6639 mL
40 mM 0.0799 mL 0.3996 mL 0.7992 mL 1.9979 mL
50 mM 0.0639 mL 0.3197 mL 0.6393 mL 1.5983 mL
H2O 60 mM 0.0533 mL 0.2664 mL 0.5328 mL 1.3319 mL
80 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9989 mL
100 mM 0.0320 mL 0.1598 mL 0.3197 mL 0.7992 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Molindone (hydrochloride)
Art. -Nr.:
HY-B1017
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