Table 2 Results of the in vitro patch clamp assay for the developed piperidine analogs in terms of the three monitored Kv1.3 current across time. Chemical structure diversity denotes; ar = aryl ring, r = aliphatic scaffold, x = spacer type and saturation.

From: Design and synthesis of novel small molecules targeting the Kv1.3 voltage-gated potassium ion channel

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Compound

Code

Chemical Structure

% remaining activity

(mean ± SD; n = 3 at 10 µM)

Ar

R

X

Peak current amplitude (PCA)

Area under curve–charge (AUC)

Relative time constant (RTC)

10a

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4-OMe

-CH = CH-

92.14 ± 1.87

82.49 ± 5.92*

79.51 ± 2.04

10b

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4-OMe

-CH2-CH2-

96.45 ± 3.00

85.08 ± 6.23

82.52 ± 4.02

10c

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4-OMe

-CH2-CH2-

87.48 ± 1.40**

62.12 ± 7.16***

65.24 ± 9.45***

10d

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4-OMe

-CH2-CH2-

98.51 ± 1.50

74.53 ± 2.16***

73.64 ± 7.53*

10e

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H

-CH2-CH2-

93.24 ± 4.35

69.28 ± 4.50***

70.45 ± 3.89**

  1. All data were done in triplicates (n = 3) and presented as Mean ± SD. One-way analysis of variance (ANOVA) plus Dunnett’s post hoc test was used for statistical comparisons. Statistical significance was set at *P < 0.05, **P < 0.01, and ***P < 0.001 for tested molecules against the vehicle samples.
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