Disease relevance of Pglu sph

• Neither Sendide nor L703,606 pretreatment resulted in a significant inhibition of the MO-induced edema in the masseter muscle [1].
• Hyperalgesia elicited by nociceptin was inhibited dose-dependently by i.t. co-administration of tachykinin NK1 receptor antagonists, CP-99,994 and sendide [2].

Psychiatry related information on Pglu sph

• The effect of SP(1-11), SP(5-11) heptapeptide, SP(6-11) hexapeptide, and SP(1-4) tetrapeptide on the circadianly organized locomotor activity was researched after i.p. application at 11 a.m. (light phasis, low activity of rats) or 7 p.m. (dark phasis, high activity) [3].

High impact information on Pglu sph

• The neurokinin-1 receptor antagonist, sendide, exhibits antinociceptive activity in the formalin test [4].
• The antinociceptive activities of sendide, an antagonist of NK1 receptors, and its analogue, [D-Trp7]sendide have been examined after intrathecal (i.t.) administrations in the mouse paw formalin test [4].
• Even highest doses (4000 pmol sendide and 8000 pmol [D-Trp7]sendide) examined, there was no motor paralysis of the hindlimbs [4].
• Prophylactic treatment with Sendide, a highly selective antagonist of the neurokinin-1 receptor, or CGRP, but not the CGRP antagonist CGRP(8-37), inhibited the development of airway inflammation and AHR in RSV-infected animals [5].
• Independently from the projections, the SP response was reduced by sendide and MEN 10,376 and mimicked by a combination of [Sar(9)-Met(O(2))(11)]SP and alpha-neurokinin [6].

Biological context of Pglu sph

• These results may indicate that the critical factor providing potency to SP(6-11) analogues is mostly related to conformational rather than hydrophilicity aspects of the molecular structure [7].

Anatomical context of Pglu sph

• Sendide is a selective and extremely potent antagonist of neurokinin-1 (NK1) receptors in the mouse spinal cord [4].
• Sendide potently displaced [3H]-labeled substance P (SP) binding to mouse spinal cord membranes in a competitive manner [8].
• Since sendide does not penetrate the central nervous system, these results suggest that the antiemetic effects of sendide are due to the inhibition of NK1 and 5-HT3 receptors on the emetic peripheral detector sites [9].
• The influence in vitro of SP and C-terminal fragments of analogues SP(5-11) (pyroGlu5, Tyr8); SP(6-11) (pyroGlu6, Tyr8); SP(6-11) (pyroGlu6, D-Phe7); SP(6-11) (pyroGlu6, D-Phe8) on the (Ca, Mg) and (Na, K) ATPases activities from synaptosomal membranes of cerebral cortex and hippocampus of rat brain were compared [10].

Associations of Pglu sph with other chemical compounds

• Therapeutic treatment with CGRP, but not CGRP(8-37) or Sendide, abolished AHR in RSV-infected animals despite increased substance P levels and previously established airway inflammation [5].
• 4. The NK1 receptor antagonists, CP-96,345, CP-99,994 and sendide, inhibited nociceptin-induced behavioural response in a dose-dependent manner [11].
• The tachykinin NK(1) receptor antagonists, (+)-[(2S,3S)-3-(2-methoxy-benzyl-amino)-2-phenylpiperidine] (CP-99,994), and [Tyr(6), D-Phe(7), D-His(9)]substance P-(6-11) (sendide), inhibited histamine-induced hyperalgesic response in a dose-dependent manner [12].
• The peptide NK1-receptor antagonists, sendide and [D-Trp7]sendide, have been evaluated for antinociceptive activity in the capsaicin test [13].
• The behavioural response elicited by other tachykinin NK1 receptor agonists, physalaemin and septide, was also reduced significantly by a small dose (1.0 pmol) of sendide [14].

Gene context of Pglu sph

• Opioid activity of sendide, a tachykinin NK1 receptor antagonist [14].
• Large doses of sendide were needed to reduce the action of neurokinin A, D-septide, neurokinin B and eledoisin [8].
• Sendide, a tachykinin NK(1) receptor antagonist, inhibited histamine-induced nociceptive behavior in the histidine decarboxylase knockout mice [15].
• The change from pre-injection level in the afferent nerve activity induced by substance P (1 microg/kg, i.v.) (453.7 +/- 51.5%) was significantly reduced by pretreatment with either sendide (100 microg/kg, i.v.) (276.1 +/- 50.1%, P < 0.05) or granisetron, a 5-HT3 receptor antagonist (1 mg/kg, i.v.) (146.3 +/- 14.0%, P < 0.01) [9].
• Antiemetic effects of sendide, a peptide tachykinin NK1 receptor antagonist, in the ferret [9].

Analytical, diagnostic and therapeutic context of Pglu sph

• The behavioural response induced by substance P was significantly inhibited by simultaneous intrathecal injection of a tachykinin NK1 receptor antagonist, [Tyr6,D-Phe7,D-His9]substance P-(6-11) (sendide), and a non-peptide antagonist, [(2S,3S)-cis-2-(di-phenylmethyl)-N-[(2- methoxyphenyl)-methyl]-1-azabicyclo[2.2.2]octan-3-amine](CP-96,345) [16].

References