Structure-activity relationship in the effects of delta-sleep-inducing peptide (DSIP) on rat sleep

Pharmacology, Biochemistry, and Behavior
F ObálB Penke

Abstract

DSIP and its analogues, [D-Trp1]-DSIP, [D-Tyr1]-DSIP, and [D-Trp1]-DSIP1-6, were injected ICV (7 nmol/kg) into rats at dark onset, and the sleep-wake activity was recorded during the 12-hr dark period and the subsequent 12-hr light period. The effects were evaluated with respect to baseline records obtained after artificial CSF injections. DSIP did not increase sleep, whereas both [D-Trp1]-DSIP and [D-Tyr1]-DSIP promoted sleep in the first part of the night. [D-Trp1]-DSIP1-6 had a prompt arousing effect. It is suggested that the sleep-promoting analogues act by facilitating slight endogenous sleep tendencies at some time after dark onset, while DSIP is degraded quickly and is therefore not effective. The increase of W after [D-Trp1]-DSIP1-6 may indicate that DSIP contains a fragment with an arousing effect. The results corroborate the notion that the active DSIP molecule has a pseudo-cyclic structure.

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Citations

Jul 27, 2011·Rossiĭskii fiziologicheskiĭ zhurnal imeni I.M. Sechenova·Iu F Pastukhov, I V Ekimova
Nov 1, 1986·Peptides·M V Graf, A J Kastin
Sep 2, 2003·Peptides·Zhongjie SunMelvin Fregly
Mar 17, 2006·Journal of Neurochemistry·Vladimir M Kovalzon, Tatyana V Strekalova
Dec 8, 2006·Expert Opinion on Therapeutic Targets·Seiji Nishino, Nobuhiro Fujiki
Jul 5, 2001·European Journal of Anaesthesiology·B J Pollard, C J Pomfrett
Oct 21, 2020·Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova·V M Kovalzon, Yu V Panchin

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