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β1-selective adrenergic receptor agonist
Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
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Serotonin 5HT3-receptor antagonist
Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
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CGRP1 receptor antagonist
Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
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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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CaSR antagonist
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
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5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
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5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
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beta-adrenergic agonist
Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent.
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D2DR inhibitor
Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
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5-HT7 receptor antagonist
SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors.
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dopamine D2 receptor agonist
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
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Adrenergic alpha-1 agonist
Midodrine hydrochloride is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. It improves clinical outcome of chronic hypotension.
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NK3 receptor 拮抗剂
Talnetant Hydrochloride是一种有效且选择性的NK3受体拮抗剂(ki = 1.4 nM,hNK-3-CHO);对hNK-3受体的选择性是对hNK-2受体的100倍,在浓度高达100 uM时对hNK-1没有亲和力。
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D3/D2 Dopamine Receptor 拮抗剂
Cariprazine hydrochloride是一种新型的抗精神病药物,对多巴胺D3(Ki = 0.09 nM)和D2(Ki = 0.5 nM)受体具有高选择性和亲和力,对5-羟色胺5-HT(1A)受体具有中等亲和力。
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Dapoxetine hydrochloride是通过抑制5-羟色胺转运蛋白,增加5-羟色胺在突触后裂隙中的作用并因此促进射精延迟而起作用。
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dopamine transporter/norepinephrine transportertransporters inhibitor
Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
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dopamine D2/D3 receptor antagonist
Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
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5-HT1B receptor antagonist
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
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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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Smo receptor agonist
SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
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GPR88 receptor agonist
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
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Adenosine deaminase inhibitor
EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts.
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dopamine D2 receptor antagonist
Risperidone hydrochloride is a serotonin 5-HT2 receptor blocker and a potent dopamine D2 receptor antagonist, with Kis of 0.16, 1.4 nM for 5-HT2 and D2 receptor, respectively.
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5-HT2C receptor antagonist
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
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5-HT2 antagonist
Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.
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5-HT (serotonin)/dopamine receptor antagonist
Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
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5-HT6 receptor antagonist
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
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β-adrenergic receptor antagonist
Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma.
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5-HT1A receptor antagonist
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
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alpha-1 adrenergic agonist
Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction.
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SphK2 抑制剂
K145 hydrochloride是选择性鞘氨醇激酶2(SphK2)抑制剂和抗癌剂。
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dopamine D2 receptor 激动剂
UNC 9994 hydrochloride,独特的,β-arrestin偏向的功能选择性多巴胺D2受体(D2R)激动剂(Ki值为30 nM;在ε-arrestin-2募集试验中EC50值为50 nM),在体内具有抗精神病活性。UNC9994在野生型小鼠中显着抑制了PCP诱导的超运动,而在Δr-arrestin-2基因敲除小鼠中这种作用被完全消除。
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- Anika Mann, .et al. New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D 2 receptor regulation and signaling, Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
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ST-836 hydrochloride是多巴胺受体配体;反帕金森氏剂。
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imidazoline receptor 1 激动剂
Moxonidine Hydrochloride (BDF5895)是咪唑啉1型受体(I1-R)选择性激动剂,为降压剂。
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5-HT1A receptor 拮抗剂
NAD 299 hydrochloride (Robalzotan)是一种选择性的,高亲和力的5-HT1A受体拮抗剂(体外Ki = 0.6 nM)。
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serotonin 2C receptor 激动剂
lorcaserin hydrochloride (APD-356)是血清素2C受体激动剂,可指示与减少热量饮食和增加体育锻炼以减轻慢性体重成人管理。
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- Li Li, .et al. Delineating a serotonin 1B receptor circuit for appetite suppression in mice, J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
- Henrik H. Hansen, .et al. Whole-brain activation signatures of weight-lowering drugs, Mol Metab, 2021, May;47:101171 PMID: 33529728
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5-HT2/5-HT1 拮抗剂
Mianserin hydrochloride是5-HT2/5-HT1拮抗剂。对5-HT6非选择性5-HT2受体拮抗剂具有中等亲和力。对5-HT6具有中等亲和力。
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μ-opioid receptor (MOR) antagonist
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist.
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5-HT1F agonist
LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
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mu-opioid receptor agonist
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
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β2-adrenergic receptor agonist
Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
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Dopamine D2 antagonist
Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.
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antihistamine
Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class.
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5-HT1F 激动剂
LY 334370 hydrochloride是一种选择性的5-HT1F受体激动剂(Ki值为1.87、16.4,> 100 (IC50))。CAS:199673-74-0(LY 334370盐酸盐);182563-08-2(LY 334370游离碱)
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dopaminergic stabilizer
ACR 16 hydrochloride是一种多巴胺能稳定剂(对于D2(低)和D2(高),Ki值分别为17550 nM和7521),通过功能性多巴胺D2受体拮抗作用和皮质谷氨酸功能的双重作用,稳定地稳定精神运动活动。在各种情况下神经传递受到干扰。
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CXCR4 拮抗剂
在CXCR4 125I-SDF抑制结合试验中,AMD-070 HCl是一种有效的选择性CXCR4拮抗剂,IC50值为13 nM,抑制T-4型HIV-1(NL4.3株)在MT-4细胞中的复制和PBMC。
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α2- adrenoceptor 拮抗剂 / I2 imidazoline receptor 激动剂
Idazoxan hydrochloride 是α2-AR肾上腺素受体拮抗剂和潜在I2咪唑啉受体激动剂。还显示I1咪唑啉受体拮抗剂活性。(I1、I2和α的公钥基础设施值分别为5.90、7.22、8.01、7.43和7.7)。
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Adrenergic α1 Receptor 拮抗剂
HEAT hydrochloride (BE 2254)是一种选择性很强的α1-肾上腺素受体拮抗剂,是3-[125I]-衍生物的前体。肾上腺素受体或肾上腺素能受体是参与多种交感神经系统过程的G蛋白偶联受体。
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dopamine receptor 激动剂
Nalmefene hydrochloride是opioid receptor拮抗剂。
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- Mark G Papich, .et al. Naloxone and nalmefene absorption delivered by hollow microneedles compared to intramuscular injection, Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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Clenbuterol hydrochloride一种拟交感神经药β2-肾上腺素受体激动剂,已被用作支气管扩张药,用于治疗肺部疾病,例如哮喘。 在较高剂量下,克仑特罗起合成代谢类固醇的作用,有利于骨骼肌蛋白质的合成,但以脂肪沉积为代价。
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- Younian Xu, .et al. Clenbuterol, a Selective β2-Adrenergic Receptor Agonist, Inhibits or Limits Post-Stroke Pneumonia, but Increases Infarct Volume in MCAO Mice, J Inflamm Res, 2022, Jan 14;15:295-309 PMID: 35058704