- 関
- NK-3 receptor
WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
UpToDate Contents
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English Journal
- The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study.
- Litman RE1, Smith MA, Desai DG, Simpson T, Sweitzer D, Kanes SJ.Author information 1From *CBH Health, LLC, Rockville, MD; †Georgetown University, Washington, DC; and ‡AstraZeneca, Wilmington, DE.AbstractProblems with the efficacy of second-generation antipsychotics on negative symptoms and cognition have highlighted the need for further development of drugs targeting central nervous system neurotransmitter systems other than dopamine. One target in development is neurokinin 3 (NK(3)) tachykinin receptors, which are coreleased and interact with dopamine. This study investigates the efficacy, tolerability, and cognitive effects of AZD2624, a selective, orally active NK(3) receptor antagonist, in symptomatic patients with schizophrenia. Patients were randomly assigned to 1 of 3 treatment groups: AZD2624 40 mg, placebo, or olanzapine 15 mg. Treatment lasted for 28 days, and the Positive and Negative Syndrome Scale, the Clinical Global Impression Severity Scale and Improvement Scales, and cognition as assessed by CogState were used as primary outcome measures. There were no significant differences in patients treated with AZD2624 versus placebo on change in Positive and Negative Syndrome Scale total score and Clinical Global Impression Severity Scale; in addition, no change in CogState measures was found. Results of the trial do not support a role for the NK(3) antagonist AZD2624 as a therapeutic treatment for acute schizophrenia when used as monotherapy.
- Journal of clinical psychopharmacology.J Clin Psychopharmacol.2014 Apr;34(2):199-204. doi: 10.1097/JCP.0000000000000071.
- Problems with the efficacy of second-generation antipsychotics on negative symptoms and cognition have highlighted the need for further development of drugs targeting central nervous system neurotransmitter systems other than dopamine. One target in development is neurokinin 3 (NK(3)) tachykinin rec
- PMID 24525659
- Molecular recognition of tachykinin receptor selective agonists: insights from structural studies.
- Ganjiwale A, Cowsik SM1.Author information 1School of Life Sciences, Jawaharlal Nehru University, New Delhi-110067. scowsik@gmail.com.AbstractThis Review deals essentially with the elucidation of structural features of Tachykinin family of neuropeptides, which are known to interact through three distinct GPCR subtypes, namely NK1 (Neurokinin 1), NK2 (Neurokinin 2) and NK3 (Neurokinin 3) receptors. In mammals, Tachykinins have been shown to elicit a wide array of activities such as powerful vasodilatation, hypertensive action and stimulation of extravascular smooth muscle and are known to be involved in a variety of clinical conditions including chronic pain, Parkinson's disease, Alzheimer's disease, depression, rheumatoid arthritis, irritable bowel syndrome and asthma. This broad spectrum of action of Tachykinins is attributed to the lack of selectivity of tachykinins to their receptors. All tachykinins interact with all the three-receptor subtypes with SP preferring NK1, NKA preferring NK2 and NKB preferring NK3. This lack of specificity can be accounted for by the conformational flexibility of these short, linear peptides. Hence, identification of structural features of the agonists important for receptor binding and biological activity is of great significance in unraveling the molecular mechanisms involved in tachykinin receptor activation and also in rational design of novel therapeutic agents. Understanding structure of the ligand-receptor complex and analysis of topography of the binding pocket of the tachykinin receptor is also crucial in rational design of drugs.
- Mini reviews in medicinal chemistry.Mini Rev Med Chem.2013 Dec;13(14):2036-46.
- This Review deals essentially with the elucidation of structural features of Tachykinin family of neuropeptides, which are known to interact through three distinct GPCR subtypes, namely NK1 (Neurokinin 1), NK2 (Neurokinin 2) and NK3 (Neurokinin 3) receptors. In mammals, Tachykinins have been shown t
- PMID 23937231
- Kisspeptin, neurokinin B, and dynorphin act in the arcuate nucleus to control activity of the GnRH pulse generator in ewes.
- Goodman RL1, Hileman SM, Nestor CC, Porter KL, Connors JM, Hardy SL, Millar RP, Cernea M, Coolen LM, Lehman MN.Author information 1PhD, Department of Physiology and Pharmacology, PO Box 9229, West Virginia University, Morgantown, West Virginia 26506. rgoodman@hsc.wvu.edu.AbstractRecent work has led to the hypothesis that kisspeptin/neurokinin B/dynorphin (KNDy) neurons in the arcuate nucleus play a key role in GnRH pulse generation, with kisspeptin driving GnRH release and neurokinin B (NKB) and dynorphin acting as start and stop signals, respectively. In this study, we tested this hypothesis by determining the actions, if any, of four neurotransmitters found in KNDy neurons (kisspeptin, NKB, dynorphin, and glutamate) on episodic LH secretion using local administration of agonists and antagonists to receptors for these transmitters in ovariectomized ewes. We also obtained evidence that GnRH-containing afferents contact KNDy neurons, so we tested the role of two components of these afferents: GnRH and orphanin-FQ. Microimplants of a Kiss1r antagonist briefly inhibited LH pulses and microinjections of 2 nmol of this antagonist produced a modest transitory decrease in LH pulse frequency. An antagonist to the NKB receptor also decreased LH pulse frequency, whereas NKB and an antagonist to the receptor for dynorphin both increased pulse frequency. In contrast, antagonists to GnRH receptors, orphanin-FQ receptors, and the N-methyl-D-aspartate glutamate receptor had no effect on episodic LH secretion. We thus conclude that the KNDy neuropeptides act in the arcuate nucleus to control episodic GnRH secretion in the ewe, but afferent input from GnRH neurons to this area does not. These data support the proposed roles for NKB and dynorphin within the KNDy neural network and raise the possibility that kisspeptin contributes to the control of GnRH pulse frequency in addition to its established role as an output signal from KNDy neurons that drives GnRH pulses.
- Endocrinology.Endocrinology.2013 Nov;154(11):4259-69. doi: 10.1210/en.2013-1331. Epub 2013 Aug 19.
- Recent work has led to the hypothesis that kisspeptin/neurokinin B/dynorphin (KNDy) neurons in the arcuate nucleus play a key role in GnRH pulse generation, with kisspeptin driving GnRH release and neurokinin B (NKB) and dynorphin acting as start and stop signals, respectively. In this study, we tes
- PMID 23959940
Japanese Journal
- Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
- Misu Ryosuke,Noguchi Taro,Ohno Hiroaki,Oishi Shinya,Fujii Nobutaka
- Bioorganic & medicinal chemistry 21(8), 2413-2417, 2013-04-15
- … Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). …
- NAID 120005244454
- Structure-Activity Relationship Study of Neurokinin-3 Receptor Agonists
- NOGUCHI Taro,OISHI Shinya,MISU Ryosuke,OHNO Hiroaki,YAMAMURA Takashi,OKAMURA Hiroaki,FUJII Nobutaka
- Peptide science : proceedings of the ... Japanese Peptide Symposium 2012, 189-190, 2013-03-01
- NAID 10031161597
- Chronic Peripheral Administration of Kappa-Opioid Receptor Antagonist Advances Puberty Onset Associated with Acceleration of Pulsatile Luteinizing Hormone Secretion in Female Rats
- NAKAHARA Tatsuo,UENOYAMA Yoshihisa,IWASE Akira [他],OISHI Shinya,NAKAMURA Sho,MINABE Shiori,WATANABE Youki,DEURA Chikaya,NOGUCHI Taro,FUJII Nobutaka,KIKKAWA Fumitaka,MAEDA Kei-ichiro,TSUKAMURA Hiroko
- Journal of Reproduction and Development 59(5), 479-484, 2013
- … Previous studies have shown involvement of the two neuropeptides, kisspeptin and neurokinin B (NKB), in controlling puberty onset. … The present study aimed to determine if attenuation of inhibitory dynorphin-kappa-opioid receptor (KOR) signaling triggers the initiation of puberty in normal developing female rats. …
- NAID 130003361050
Related Links
- Fig. 1. Comparison of the distribution of the NK 3 receptor protein or mRNAs encoding NK 3 receptor in the rat, guinea pig and gerbil brain. Acc = accumbens nucleus, AccS = anterior cingulate cortex; AHA = anterior hypothalamic ...
- G-protein coupled receptors (GPCR) are cell membrane proteins that are characterized by 7 membrane spanning domains, extracellular domains that bind ligands, and intracellular domains that bind G-proteins allowing regulation of ...
Related Pictures
★リンクテーブル★
[★]
- 英
- neurokinin-3 receptor、NK-3 receptor
- 関
- ニューロキニン-3受容体、ニューロキニン3レセプター、ニューロキニン-3レセプター、NK-3受容体、NK-3レセプター
[★]
- 英
- neurokinin-3 receptor
- 関
- ニューロキニン-3受容体、ニューロキニン3受容体、ニューロキニン-3レセプター
[★]
- 英
- neurokinin-3 receptor
- 関
- ニューロキニン-3受容体、ニューロキニン3受容体、ニューロキニン3レセプター
[★]
- 関
- neurokinin-3 receptor