Tachykinin NK1 Receptor Antagonists

Patacchini, Riccardo; Maggi, C.A.

doi:10.1007/978-3-642-18891-6_6

Cited by 3 publications

(3 citation statements)

References 175 publications

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“…For example, at least 2 subtypes of the NK1 receptor are known, the "classical" and "septide" types, which have different distribution in various species. Bioassays assessing the NK receptor-blocking ability of different antagonists showed variable potency among species, based on preference for the receptor subtype (Patacchini and Maggi, 2004). Heterogeneity of NK2 and NK3 receptors is also likely to exist (reviewed in Maggi, 1995).…”

Section: Discussionmentioning

confidence: 99%

“…In recent years, a number of selective NK agonists and/or antagonists have been developed as potential therapeutic agents and there is considerable literature describing their pharmacology (reviewed in Patacchini and Maggi, 2004; Emonds-Alt, 2004; Mazzone and Canning, 2004; Rumsey and Kerns, 2004). However, there are no previous reports of reproductive toxicity in dogs or other species associated with any of these agents.…”

Section: Discussionmentioning

confidence: 99%

“…For example, RP67580, an NK1 antagonist, was found to be 10–20-fold more potent in blocking NK1 receptors in rats as compared to those in guinea pigs or humans. In contrast, CP96345 was 30–100-fold more potent in humans, guinea pigs, and dogs than in rats or mice (Patacchini and Maggi, 2004). Differences in the pharmacologic action of these drugs between species have been linked to discrete point mutations on the human and rat NK1 receptors that affect binding affinity (Fong et al, 1992).…”

Section: Discussionmentioning

confidence: 99%

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Administration of an Antagonist of Neurokinin Receptors 1, 2, and 3 Results in Reproductive Tract Changes in Beagle Dogs, but Not Rats

Losco¹,

Leach²,

Sinha³

et al. 2007

Toxicol Pathol

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SCH 206272, an antagonist of neurokinin receptors 1, 2, and 3, was administered orally by gavage for 1 month to 8-to 10-month-old dogs at doses of 0, 15, 30, or 60 mg/kg, and to 6-week-old rats at doses of 0, 30, 100, or 300 mg/kg. The most important changes occurred in the reproductive tract of the dogs at all doses. Absolute and relative group mean organ weights for the testes, prostate gland, epididymides, ovaries, and uterus were 33-86% lower than concurrent controls in groups receiving SCH 206272. Organ weight changes were not dose-related. Microscopic changes that correlated with the organ weight changes occurred in all groups receiving SCH 206272. For males, they included minimal to severe atrophy of the testes, epididymides, and prostate gland. In addition, the epididymides exhibited severe oligospermia or aspermia, minimal epithelial apoptosis and mild epithelial vacuolation. In female dogs, the ovaries and uteri appeared immature. Microscopic changes were similar in incidence and severity in dogs receiving 30 or 60 mg/kg, but were slightly less in dogs receiving 15 mg/kg. In contrast, similar findings were not observed in the reproductive tract of male or female rats, despite overlapping systemic, hypothalamic, and pituitary gland concentrations of SCH 206272.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Administration of an Antagonist of Neurokinin Receptors 1, 2, and 3 Results in Reproductive Tract Changes in Beagle Dogs, but Not Rats

Losco¹,

Leach²,

Sinha³

et al. 2007

Toxicol Pathol

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Chronic Restraint Stress Inhibits Hair Growth via Substance P Mediated by Reactive Oxygen Species in Mice

et al. 2013

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BackgroundsSolid evidence has demonstrated that psychoemotional stress induced alteration of hair cycle through neuropeptide substance P (SP) mediated immune response, the role of reactive oxygen species (ROS) in brain-skin-axis regulation system remains unknown.ObjectivesThe present study aims to investigate possible mechanisms of ROS in regulation of SP-mast cell signal pathway in chronic restraint stress (CRS, a model of chronic psychoemotional stress) which induced abnormal of hair cycle.Methods and ResultsOur results have demonstrated that CRS actually altered hair cycle by inhibiting hair follicle growth in vivo, prolonging the telogen stage and delaying subsequent anagen and catagen stage. Up-regulation of SP protein expression in cutaneous peripheral nerve fibers and activation of mast cell were observed accompanied with increase of lipid peroxidation levels and reduction of the activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in CRS mice skin. In addition, SP receptor antagonist (RP67580) reduced mast cell activations and lipid peroxidation levels as well as increased GSH-Px activity and normalized hair cycle. Furthermore, antioxidant Tempol (a free radical scavenger) also restored hair cycle, reduced SP protein expression and mast cell activation.ConclusionsOur study provides the first solid evidence for how ROS play a role in regulation of psychoemotional stress induced SP-Mast cell pathway which may provide a convincing rationale for antioxidant application in clinical treatment with psychological stress induced hair loss.

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Neurokinin-3 receptor antagonists in schizophrenia

Albert¹,

Potts

2006

Expert Opinion on Therapeutic Patents

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Tachykinin NK1 Receptor Antagonists

Cited by 3 publications

References 175 publications

Administration of an Antagonist of Neurokinin Receptors 1, 2, and 3 Results in Reproductive Tract Changes in Beagle Dogs, but Not Rats

Administration of an Antagonist of Neurokinin Receptors 1, 2, and 3 Results in Reproductive Tract Changes in Beagle Dogs, but Not Rats

Chronic Restraint Stress Inhibits Hair Growth via Substance P Mediated by Reactive Oxygen Species in Mice

Neurokinin-3 receptor antagonists in schizophrenia

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