Positive modulators of N -methyl- d -aspartate receptor: structure–activity relationship study on steroidal C-17 and C-20 oxime ethers

Santosh Kumar Adla; Barbora Hrčka Krausová; Bohdan Kysilov; Karel Kudláček; Radko Souček; Milos Budesinsky; Jan Voldřich; Ladislav Vyklický; Eva Kudová

doi:10.1039/d5ra07716h

January 1, 2026RSC AdvancesOpen Access

Positive modulators of N -methyl- d -aspartate receptor: structure–activity relationship study on steroidal C-17 and C-20 oxime ethers

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Key Points

To investigate the structure-activity relationships of steroidal C-17 and C-20 oxime ethers as positive modulators of NMDAR.
Evaluated the potency and efficacy of pregnenolone C-20 oxime ethers compared to pregnenolone sulfate.
Utilized bioisosteric design principles to develop and assess new neurosteroid derivatives.
Pregnenolone C-20 oxime ethers demonstrated higher potency and efficacy than pregnenolone sulfate.
The study validates the D-ring bioisosteric design strategy in enhancing the neurosteroid properties.

Implication

A structure-activity relationship study reveals that pregnenolone C-20 oxime ethers enhance NMDAR activity, suggesting a new strategy for neurosteroids.

Abstract

Pregnenolone C-20 oxime ethers are highly potent NMDAR PAM neurosteroids, outperforming pregnenolone sulfate in efficacy, potency, and drug-like properties, validating D-ring bioisosteric design as a promising strategy.

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Cite This Study

Adla et al. (2026) studied this question.

synapsesocial.com/papers/699fe34695ddcd3a253e70ab https://doi.org/10.1039/d5ra07716h

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Positive modulators of N -methyl- d -aspartate receptor: structure–activity relationship study on steroidal C-17 and C-20 oxime ethers

Key Points

Implication

Abstract

Discussion

Cite This Study

Positive modulators of N -methyl- d -aspartate receptor: structure–activity relationship study on steroidal C-17 and C-20 oxime ethers

Key Points

Implication

Abstract

Discussion

Cite This Study

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