目录号 | 产品详情 | 靶点 | |
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T37373 | |||
4-hydroxy-3-Methoxyphenylglycol (piperazine salt) is a metabolite of norepinephrine derived in part by deamination of normetanephrine or by O-methylation of dihydroxyphenylglycol after cellular uptake of either intermediate. It is released into the blood and cerebrospinal fluid and has been used as a biochemical index of recent sympathetic nervous system activity. | |||
T3S0964 | Others | ||
Chrysoeriol-7-O-glucoside can strongly inhibit the classical pathway of the complement system.Chrysoeriol-7-O-d-glucoside and luteolin-7-O-d-glucoside can inhibit palmitic acid uptake into small intestinal brush border membrane, apigenin-7-O-d-glucoside can inhibit alpha-amylase activity; they can enhance norepinephrine-induced lipolysis in fat cells. | |||
T15455 | Others | ||
RGH-5526是一种新型的抗高血压药。它引起下丘脑去甲肾上腺素(NA)周转(利用)增加,下丘脑去甲肾上腺素能神经元活性的增加可能导致外周交感神经活性的降低,从而显著降低血压。 | |||
T60508 | |||
(S)-Venlafaxine 是 Venlafaxine 的(S)-构型。Venlafaxine 是一种具有口服活性的 5-羟色胺 (5-HT)/去甲肾上腺素 (NE) 再摄取双重抑制剂, 具有抗抑郁活性。 | |||
T7073 | |||
Milnacipran 是5-羟色胺-去甲肾上腺素重吸收抑制剂(SNRI),临床上可用于纤维肌痛治疗。Milnacipran 口服后吸收良好,生物利用度为 85%。 | |||
T37211 | |||
5-hydroxy-6-methoxy (S)-Duloxetine is a metabolite of (S)-duloxetine . It is formed from (S)-duloxetine via a 5- or 6-hydroxy duloxetine intermediate, which is formed by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6, and a catechol duloxetine intermediate. 5-hydroxy-6-methoxy (S)-Duloxetine binds to the serotonin (5-HT), norepinephrine, and dopamine transporters with Ki values of 266, 920, and 2,814 nM, respectively. | |||
T37794 | |||
Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997). | |||
T30108 | |||
Aptazapine (CGS 7525A) is a tetracyclic antidepressant (TECA) that is a potent α2-adrenergic receptor antagonist and has also been shown to act as a 5-HT2 receptor antagonist and an H1 receptor reverse agonist, both for serotonin reuptake or norepinephrin | |||
T70487 | |||
Tofenacin (free base) is an antidepressant drug with a tricyclic-like structure. It acts as a serotonin-norepinephrine reuptake inhibitor, and based on its close relation to orphenadrine, may also possess anticholinergic and antihistamine properties. Tofenacin is also the major active metabolite of orphenadrine and likely plays a role in its beneficial effects against depressive symptoms seen in Parkinson's disease patients. | |||
T73977 | |||
(S)-Dehydro Venlafaxine 是 Dehydro Venlafaxine 的非活性 S-对映异构体。Dehydro Venlafaxine 是 Venlafaxine 的杂质。Venlafaxine (Wy 45030) 是有效的 5-羟色胺 (5-HT) / 去甲肾上腺素 (NE) 再摄取双重抑制剂。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03852 | Dopamine beta-Hydroxylase Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
DBH is a 29 kDa copper-containing oxygenase. It can be detected in noradrenergic nerve terminals of the central and peripheral nervous systems, and is also expressed in chromaffin cells of the adrenal medulla. DBH contains our identical subunits, and its activity requires ascorbate as a cofactor. It functions in in the synthesis of small-molecule neurotransmitters that is membrane-bound, making norepinephrine the only transmitter synthesized inside vesicles. DBH has been shown to be associated with decision making and addictive behaviors such as alcohol and smoking, attention deficit hyperactivity disorder, and also with neurological diseases such as Schizophrenia and Alzheimer's.
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TMPY-02948 | SULT1A3 Protein, Human, Recombinant (His) | Human | E. coli | ||
SULT1A3 belongs to the sulfotransferase 1 family. Sulfotransferase enzymes catalyze the sulfate conjugation of many hormones, neurotransmitters, drugs, and xenobiotic compounds. They are different in their tissue distributions and substrate specificities while their gene structure (number and length of exons) is similar. SULT1A3 gene encodes a phenol sulfotransferase with thermolabile enzyme activity. Four sulfotransferase genes are located on the p arm of chromosome 16; this gene and SULT1A4 arose from a segmental duplication. It is the most centromeric of the four sulfotransferase genes. Exons of this gene overlap with exons of a gene that encodes a protein containing GIY-YIG domains (GIYD1). SULT1A3 is expressed in liver, colon, kidney, lung, brain, spleen, small intestine, placenta and leukocyte. SULT1A3 is a sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs.
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