cas 2565-01-7, (6aS)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-benzo[de][1,3]benzodioxolo[5,6-g]quinoline

Articles about 2565-01-7Total 2 be found

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Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine
The naturally occurring aporphine alkaloid nantenine, has been shown to antagonize behavioral and physiological effects of MDMA in mice. We have synthesized (±)-nantenine via an oxidative cyclization reaction with PIFA and evaluated its binding profile against a panel of CNS targets. To begin to understand the importance of the chiral center of nantenine with regards to its capacity to antagonize the effects of MDMA in vivo, (R)- and (S)-nantenine were prepared and evaluated in a food-reinforced operant task in rats. Pretreatment with either nantenine enantiomer (0.3 mg/kg ip) completely blocked the behavioral suppression induced upon administration of 3.0 mg/kg MDMA. (±)-Nantenine displayed high affinity and selectivity for the α1A adrenergic receptor among several other receptors suggesting that this α1 subtype may be significantly involved in the anti-MDMA effects of the enantiomers.
LeGendre, Onica,Pecic, Stevan,Chaudhary, Sandeep,Zimmerman, Sarah M.,Fantegrossi, William E.,Harding, Wayne W.
p. 628 - 631
(2010)
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Evaluation of structural effects on 5-HT2A receptor antagonism by aporphines: Identification of a new aporphine with 5-HT2A antagonist activity
A set of aporphine analogs related to nantenine was evaluated for antagonist activity at 5-HT2A and α1A adrenergic receptors. With regards to 5-HT2A receptor antagonism, a C2 allyl group is detrimental to activity. The chiral center of nantenine is not important for 5-HT2A antagonist activity, however the N6 nitrogen atom is a critical feature for 5-HT2A antagonism. Compound 12b was the most potent 5-HT2A aporphine antagonist identified in this study and has similar potency to previously identified aporphine antagonists 2 and 3. The ring A and N6 modifications examined were detrimental to α1A antagonism. A slight eutomeric preference for the R enantiomer of nantenine was observed in relation to α1A antagonism.
Ponnala, Shashikanth,Gonzales, Junior,Kapadia, Nirav,Navarro, Hernan A.,Harding, Wayne W.
p. 1664 - 1667
(2014/04/17)

Chemical Properties

Boiling Point: 487.5°Cat760mmHg
Flash Point:145.2°C
Density: 1.266g/cm³
Vapor Pressure: 1.18E-09mmHg at 25°C
PSA: 40.16000
LogP: 3.12250

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2565-01-7

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Chemical Properties

Boiling Point: 487.5°Cat760mmHg

Flash Point:145.2°C

Density: 1.266g/cm³

Vapor Pressure: 1.18E-09mmHg at 25°C

PSA: 40.16000

LogP: 3.12250

Global suppliers and manufacturers of 2565-01-7total 7 suppliers on LookChem

Article Database

2565-01-7

Articles about 2565-01-7Total 2 be found

More Articles about upstream products of 2565-01-7

Chemical Properties

Boiling Point: 487.5°Cat760mmHg

Flash Point:145.2°C

Density: 1.266g/cm3

Vapor Pressure: 1.18E-09mmHg at 25°C

PSA: 40.16000

LogP: 3.12250

Global suppliers and manufacturers of 2565-01-7total 7 suppliers on LookChem

Density: 1.266g/cm³