Table Info

Table 1.

Antagonist activity of β-lactams 1a–d and analogue 9d at rTRPM8 channels in microfluorometry assays and patch-clamp experiments

Compound	R	Configuration	Ca²⁺ microfluorometry		Patch clamp
Compound	R	Configuration	IC₅₀ (µM)	95% confidence intervals	IC₅₀ (µM)	95% confidence intervals
1a	O^tBu	3S,4S,2'S	1.06 ± 1.21	0.72 to 1.55	0.97 ± 1.56	0.38 to 2.45
1b	O^tBu	3S,4S,2'R	0.72 ± 0.12	0.64 to 0.80	1.21 ± 0.4	0.82 to 1.72
1c	O^tBu	3R,4R,2'S	4.48 ± 0.80	3.62 to 5.56	2.94 ± 0.75	2.27 to 3.69
1d	O^tBu	3R,4R,2'R	5.02 ± 1.50	3.76 to 6.77	3.34 ± 0.8	2.40 to 5.52
9d	NHⁱBu	3R,4R,2'R	0.41 ± 0.10	0.36 to 0.46	0.90 ± 1.25	0.57 to 1.42
AMTB	NA	ND	7.3 ± 1.5	8.82 to 7.85	ND	ND

ND: no determined; NA: not applicable; AMTB: N-(3-aminopropyl)-2-[(3-methylphenyl)methoxy]-N-(2-thienylmethyl)benzamide hydrochloride; IC₅₀: concentration exerting a half-maximal inhibition; rTRPM8: rat transient receptor potential melastatin channel, subtype 8; R: substituent at the 4-position; O^tBu: tert-butyl ester; NHⁱBu: N-isobutyl amide

Supplementary materials

The supplementary materials for this article are available at: https://www.explorationpub.com/uploads/Article/file/100882_sup_1.pdf.

Declarations

Acknowledgments

We thank Jessy Medina for technical assistance.

Author contributions

CME and TV: Investigation, Formal analysis, Writing—review & editing. MAB and AMP: Investigation, Writing—review & editing. AFM: Supervision, Funding acquisition, Writing—review & editing. AFC: Supervision, Funding acquisition, Writing—original draft, Writing—review & editing. RGM: Conceptualization, Supervision, Funding acquisition, Writing—original draft, Writing—review & editing. All authors read and approved the submitted version.

Conflicts of interest

Rosario González-Muñiz, the Editorial Board Member of Exploration of Drug Science and Guest Editor of the special issue—Mimicking Nature: Biomimetics as Tools for Diagnosis and Therapeutics, had no involvement in the journal review process of this manuscript. The other authors declare that they have no conflicts of interest.

Ethical approval

Animal experimentation procedures were conducted under the approval of the Institutional Animal and Ethical Committee at UMH (UMH.IDI.AFM.06.20), and approved by the Generalitat Valenciana (2021/VSC/PEA/0089).

Consent to participate

Not applicable.

Consent to publication

Not applicable.

Availability of data and materials

Most data from this paper are included in this manuscript and the supplementary materials. Additional data could be obtained from the authors upon request.

Funding

This research was funded by FEDER [MCIN/AEI/10.13039/501100011033]; Una manera de hacer Europa [PID2021-126423OB-C21, to AFM and AFC], [PID2021-126423OB-C22, to RGM]; Generalitat Valenciana [PROMETEO/2021/031, to AFM]; CSIC [202180E073, to RGM]; and Comunidad de Madrid [IND2017/BMD7673, to RGM]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.

Copyright

Publisher’s note

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