Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H26N4O4S |
| Molecular Weight | 454.542 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCN(CC1=CN=CC=C1)C(=O)CN(C2=CN=C(OC)C=C2)S(=O)(=O)C3=CC=CC=C3C
InChI
InChIKey=KJPHTXTWFHVJIG-UHFFFAOYSA-N
InChI=1S/C23H26N4O4S/c1-4-26(16-19-9-7-13-24-14-19)23(28)17-27(20-11-12-22(31-3)25-15-20)32(29,30)21-10-6-5-8-18(21)2/h5-15H,4,16-17H2,1-3H3
| Molecular Formula | C23H26N4O4S |
| Molecular Weight | 454.542 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulphonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA) is a high-affinity, reversible and selective orexin type 2 (OX2) receptor antagonist. The in vivo activity of EMPA was assessed by reversal of orexin-B-induced hyperlocomotion during the resting phase in mice and the reduction of spontaneous locomotor activity (LMA) during the active phase in rats.
Originator
Approval Year
Sample Use Guides
Male NMRI mice: Mice were injected i.p. with EMPA (1, 3, 10, 30, 100, 300 mg·kg−1, n= 8 mice per dose).
Male Wistar rats: one hour after the dark period onset, rats were injected i.p. with EMPA (3, 10, 30 mg·kg−1, n= 8 rats per dose) and immediately placed into the activity monitoring chambers.
Route of Administration:
Intraperitoneal
The distribution and abundance of in vitro binding sites of [3H]EMPA (1 nmol·L−1), measured by quantitative autoradiography and image analysis, was investigated in coronal rat brain sections. A high density of specific binding was observed in many brain regions including the limbic cortices, hippocampus, striatum and hypothalamic nuclei. Non-specific binding (NSB), determined in the presence of 10 µmol·L−1 Cp-5, a selective OX2 receptor antagonist.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:05:59 UTC 2023
by
admin
on
Sat Dec 16 18:05:59 UTC 2023
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| Record UNII |
VT87V86D7W
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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9981404
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VT87V86D7W
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EMPA (drug)
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680590-49-2
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admin on Sat Dec 16 18:05:59 UTC 2023 , Edited by admin on Sat Dec 16 18:05:59 UTC 2023
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DTXSID101045254
Created by
admin on Sat Dec 16 18:05:59 UTC 2023 , Edited by admin on Sat Dec 16 18:05:59 UTC 2023
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> INHIBITOR |
ANTAGONIST
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TARGET -> INHIBITOR |
ANTAGONIST
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