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  • antagonist
  • Fezolinetant is an oral neurokinin-3 receptor antagonist which has been optimized for use in women's health, and is being developed for sex hormone-related disorders such as endometriosis, polycystic ovary syndrome and uterine fibroids. (imsociety.org)
  • A new treatment, called a neurokinin 3 receptor antagonist, shows promise for the future. (lubbockonline.com)
  • Ardayfio PA et al (2008) The 5-hydroxytryptamine2A receptor antagonist R-(+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat. (springer.com)
  • In rats receiving aldosterone/salt treatment (ALDOST) alone for 1 and 4 wk or in combination with spironolactone (Spiro), an ALDO receptor antagonist, we monitored 24-h urinary and fecal Zn excretion and tissue Zn levels in heart, liver, and skeletal muscle, together with tissue metallothionein (MT)-I, a Zn(2+)-binding protein, and Cu/Zn-SOD activities in plasma and tissues. (thisisms.com)
  • Potent, selective and competitive non-peptide NK 3 receptor antagonist (K i = 13 nM at hNK 3 ). (tocris.com)
  • Theoretically, an antagonist could block this biological reaction by binding to the neurokinin 3 receptor and preventing the actions of neurokinin B. (medicalxpress.com)
  • Recently, Dr. Julia Prague, along with Dhillo and colleagues, tested the neurokinin 3 receptor antagonist (MLE4901) in a phase 2, randomized, double-blind clinical trial with 68 women. (medicalxpress.com)
  • KNDy
  • The kisspeptin/neurokinin B/dynorphin (KNDy) cell population of the arcuate nucleus: sex differences and effects of prenatal testosterone in sheep. (nih.gov)
  • gene expression
  • Furthermore, menopause and/or oophorectomy are associated with changes in NKB gene expression: in the human infundibular nucleus it increases after menopause, and in monkeys and rats ovariectomy induces similar increases in NKB gene expression that are reversed by estradiol therapy [3]. (imsociety.org)
  • Pinto FM, Pintado CO, Pennefather JN, Patak E, Candenas L. Ovarian steroids regulate tachykinin and tachykinin receptor gene expression in the mouse uterus. (imsociety.org)
  • We analyzed tachykinin NK 3 receptor (NK 3 R) gene expression by semiquantitative reverse transcription-polymerase chain reaction (RT-PCR) in uteri from young (3-month-old) and old (30-month-old) rats. (aspetjournals.org)
  • Activation
  • This implies that the effects of 5-HT 2A receptor activation on the activity of L5 pyramidal cells may be responsible for mediating a range of behaviors linked to limbic circuitry with connectivity between the PFC, striatum, thalamus, claustrum, striatum, amygdala, and the hippocampal formation. (springer.com)
  • Sensitization of hypervigilance effects of cocaine can be induced by NK3 receptor activation in marmoset monkeys. (semanticscholar.org)
  • Neurokinin 3 receptor activation potentiates the psychomotor and nucleus accumbens dopamine response to cocaine, but not its place conditioning effects. (semanticscholar.org)
  • GnRH
  • Kisspeptin, neurokinin B, and dynorphin act in the arcuate nucleus to control activity of the GnRH pulse generator in ewes. (nih.gov)
  • Suppression of the GnRH pulse generator by neurokinin B involves a κ-opioid receptor-dependent mechanism. (nih.gov)
  • hypogonadism
  • OBJECTIVE : Patients with mutations of neurokinin B (NKB) and its receptor show hypogonadotrophic hypogonadism, but there is little evidence for the importance of this pathway in reproductive function in normal men, or its functional hierarchy with kisspeptin. (up.ac.za)
  • role
  • These effects on 5-HT 2A receptors and related GPCRs appear to play a major role in the behavioral effects of serotonergic hallucinogens, such as head twitches in rodents and higher order behaviors such as rodent lever pressing on the differential-reinforcement-of-low rate 72-s (DRL 72-s) schedule. (springer.com)
  • Role of neurokinin B in the control of female puberty and its modulation by metabolic status. (nih.gov)
  • mechanism
  • Beique J-C et al (2007) Mechanism of the 5-hydroxytryptamine 2A receptor-mediated facilitation of synaptic activity in prefrontal cortex. (springer.com)