“vasopressin receptor”的搜索结果
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V2R agonist
Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia.
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AMPA/kainate receptors agonist
(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
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mGluRs M3 agonist
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
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GABAA receptors agonist
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a selective agonist at GABAA receptors that contain α4-δ subunits, and has anxiolytic and sedative effects.
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group III mGluR receptors agonist
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
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GPR119 receptors agonist
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.
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5-HT1A/5-HT1B receptors agonist
RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
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peripheral oxytocin receptors agonist
Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
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excitatory transmitter/agonist
L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
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glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
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5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
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opioid receptors agonist
DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively.
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dopamine D2 autoreceptor agonist
NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
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Peripheral chemoreceptor agonist
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
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Muscarinic agonist
Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
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GABA agonist
Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission.
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mAChR agonist
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
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Serotonin receptors agonist
Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors.
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ultra-long-acting β? adrenoreceptor 激动剂
Vilanterol是一种新的选择性β2-AR激动剂,PEC50值为10.37±0.05。
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β-adrenergic receptors 激动剂
Cimaterol是β的有效激动剂;肾上腺素能受体(人β的pEC50 = 8.13、8.78和6.62;1β,2β和3β)。
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β3-adrenergic receptors 激动剂
BRL 37344 Na Salt是具有脂解活性的β3-AR(β3-肾上腺素能受体)选择性激动剂。
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Opioid Receptors 激动剂
BRL 52537 hydrochloride是一种高度选择性和有效的κ阿片类激动剂(Ki = 0.24 nM)。比吗啡强25倍。
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LXR-like receptors 激动剂
GW3965 HCl是一种选择性的口服活性肝X受体(LXR)完全激动剂。
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- Mohácsik P, .et al. A Transgenic Mouse Model for Detection of Tissue-Specific Thyroid Hormone Action, Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation., Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway, J Lipid Res., 2013, May; 54(5): 1241-1254. PMID: 23427282
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Glucocorticoid receptor agonist
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
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histamine H4 receptor inverse agonist
H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
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Orexin 2 receptor 激动剂
Orexin 2 Receptor Agonist一种有效的选择性Orexin2受体激动剂。
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TGR5(GPCR19) 激动剂
TGR5 Receptor Agonist是一种有效的TGR5(GPCR19)激动剂,在U2-OS细胞分析(pEC50 = 6.8)和黑素细胞(pEC50 = 7.5)中显示出增强的效力。
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partial dopamine D2 and D3 receptor agonist
Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.
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sigma 1 receptor agonist
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(??1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4??1.9 nM); 100-fold less affinity for the sigma 2 receptor.
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IP receptor agonist
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
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Benzodiazepine receptor/GABAA receptor agonist
U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
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D3 receptor and D2 receptor partial agonist
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
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D1-like dopamine receptor (D1/D5) agonist
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity.
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Sigma receptor agonist
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (??1/??2 receptor).
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5-HT2C receptor agonist
YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
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Androstane receptor agonist
TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR.
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nicotinic receptor agonist
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
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A1 receptor agonist
N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).
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group II (mGlu2/3) receptor agonist
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
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angiotensin-(1-7) receptor agonist
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
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GPR109a receptor agonist
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
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human 5-HT1A receptor partial agonist
Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
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dopamine D4 receptor partial agonist
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
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glucocorticoid receptor agonist
Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
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non-peptide nociceptin receptor (NOP) agonist
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
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δ opioid receptor agonist
AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2??0.9 nM for δ agonist potency.
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SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
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D1/D5 receptor full agonist
SKF 82958 is a D1/D5 receptor full agonist.
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progesterone receptor agonist
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
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ghrelin receptor inverse agonist
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
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