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[CAS NO. 475-83-2]??Nuciferine

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PRODUCTS SPECIFICATIONS [475-83-2]

Catalog
HY-N0049
Brand
MCE
CAS
475-83-2

DESCRIPTION [475-83-2]

Overview

MDLMFCD01664592
Molecular Weight295.38
Molecular FormulaC19H21NO2
SMILESCN1CCC2=CC(OC)=C(OC)C3=C2[C@@]1([H])CC4=CC=CC=C34

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


Summary

Nuciferine is an antagonist at 5-HT 2A ( IC 50 =478 nM), 5-HT 2C ( IC 50 =131 nM), and 5-HT 2B ( IC 50 =1 μM), an inverse agonist at 5-HT 7 ( IC 50 =150 nM), a partial agonist at D 2 ( EC 50 =64 nM), D 5 ( EC 50 =2.6 μM) and 5-HT 6 ( EC 50 =700 nM), an agonist at 5-HT 1A ( EC 50 =3.2 μM) and D 4 ( EC 50 =2 μM) receptor.


IC50 & Target

5-HT 2C Receptor

131 nM (IC 50 )

5-HT 7 Receptor

150 nM (IC 50 )

5-HT 2A Receptor

478 nM (IC 50 )

5-HT 2B Receptor

1 μM (IC 50 )

5-HT 6 Receptor

700 nM (EC 50 )

5-HT 1A Receptor

3.2 μM (EC 50 )

D 2 Receptor

64 nM (EC 50 )

D 4 Receptor

2 μM (EC 50 )

D 5 Receptor

2.6 μM (EC 50 )


In Vitro

Nuciferine is a partial agonist at DD 2 receptor with an activity (E max =67% of dopamine) similar to aripiprazole (E max =50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of G i with a potency similar to clozapine (Nuciferine K B =62 nM; Clozapine K B =20 nM) as determined via Schild regression analysis [1] . The natural product Nuciferine acts as an effective inhibitor of adult worm motility. Nuciferine is effective at inhibiting both basal and 5-HT evoked motility of adult schistosomes. Nuciferine inhibits Sm.5HTR L and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively [2] .

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


In Vivo

In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT 2A agonist, substituted for clozapine discriminative stimulus, enhanced amphetamine induced locomotor activity, inhibited phencyclidine (PCP)-induced locomotor activity, and rescued PCP-induced disruption of prepulse inhibition without induction of catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP doses produce similar substitution to PCP alone. In the clozapine-trained animals, a dose-dependent substitution for 1.25 mg/kg clozapine is seen at 10 mg/kg Nuciferine (80.63% drug lever responding), with an ED 50 value of 5.42 mg/kg (95% CI 3.09-9.48 mg/kg) while the lower doses tested (0.1 mg/kg-3 mg/kg) fails to produce substitution for clozapine’s discriminative cue. In addition to a high percentage of responding on the clozapine-appropriate lever, 10 mg/kg Nuciferine also produces significant rate suppression as compared to vehicle control points (p<0.001) [1] .

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


Appearance

Solid



Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL ( 16.93 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3855 mL 16.9273 mL 33.8547 mL
5 mM 0.6771 mL 3.3855 mL 6.7709 mL
10 mM 0.3385 mL 1.6927 mL 3.3855 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 1.11 mg/mL (3.76 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 1.11 mg/mL (3.76 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

4H-Dibenzo[de,g]quinoline, 5,6,6a,7-tetrahydro-1,2-dimethoxy-6-methyl-, (6aR)-
6aβ-Aporphine, 1,2-dimethoxy-
Nuciferine
4H-Dibenzo[de,g]quinoline, 5,6,6a,7-tetrahydro-1,2-dimethoxy-6-methyl-, (R)-
(6aR)-5,6,6a,7-Tetrahydro-1,2-dimethoxy-6-methyl-4H-dibenzo[de,g]quinoline
l-Nuciferine
(-)-Nuciferine
(R)-1,2-Dimethoxyaporphine
Nuciferin
D-(-)-Nuciferine
1,2-Dimethoxy-6aβ-aporphine
Sanjoinine E
(R)-Nuciferine
VLT 049
(6AR)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline

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