Proteína de Transporte Membranar

Prazosin HCl, a synthetic antiadrenergic, treats hypertension, heart failure, and more by relaxing blood vessels with an unclear mechanism.

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

<p>Dothiepin is a tricyclic antidepressant used to treat depression in patients who are not responding to alternative therapies. This drug inhibits the reuptake of norepinephrine and serotonin, increasing available neurotransmitter levels at the synaptic cleft. It also exhibits anticholinergic, antihistamine and central sedative properties.</p>

<p>Lofepramine is a psychoactive drug that belongs to the class of tricyclic antidepressants. It is used to treat depression and anxiety disorders. This drug works by inhibiting the reuptake of neurotransmitters such as serotonin and norepinephrine and as a result these neurotransmitters remain active in the brain for a longer period, which can help improve mood and alleviate symptoms of depression.</p>

<p>Inhibits P-gp transporters ; modulates P-gp-mediated multidrug resistance</p>

<p>GABA reuptake inhibitor</p>

<p>Inhibits urate anion exchanger 1 (URAT1); therapeutic use in gout</p>

<p>Agonist of mechanosensitive cation channel Piezo1, which is expressed in bladder, kidney, lung, colon and skin tissues. Yoda 1 stabilizes the Piezo1 channel in an open state and reduces the threshold for mechanical activation. Yoda 1 also partially activates the Piezo1 channel in absence of mechanical stimuli.</p>

<p>Inhibits CK1 α, δ and ε isoforms (IC50 values = 8.9, 0.5, and 4.7 μM, respectively). Induces reprogramming of epiblast-derived stem cells (EpiSCs) to embryonic stem cells (ESCs). If the latter express Oct4-GFP, the compound can be used as a tool to study this signaling pathway.</p>

Nefopam is a non-narcotic analgesic drug that has been used in the treatment of chronic pain. It belongs to the class of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). Nefopam is also a nasal drug that relieves pain by blocking neurokinin 1 receptor, which reduces the production of prostaglandins. Nefopam acts in the brain and spinal cord to relieve pain through different mechanisms such as antinociceptive effects from triple monoamine reuptake inhibition, and antihyperalgesic activity through modulation of glutamatergic transmission.

Citalopram is a selective serotonin reuptake inhibitor that is used for the treatment of depression. It has also been found to relieve and manage symptoms of anxiety, eating disorders and OCD. Citalopram targets serotonin by inhibiting its reuptake in the synaptic cleft. In vitro studies demonstrate that citalopram is a strong and selective inhibitor of neuronal serotonin reuptake and has weak effects on norepinephrine and dopamine central reuptake. .

Doxepin is a psychotropic agent that is used in the treatment of depression, anxiety and insomnia. This drug has antidepressant and anxiolytic properties. This mechanism of action for this drug is not clear however it is known to be a histamine receptor antagonist.

<p>Inhibitor of glucose uptake via GLUT1 and GLUT4 transporters, promoting intracellular glucose deprivation. The compound is a chemical sensitizer to the FAS cell death receptor and is able to break down the resistance of caspase activation. It has potential for anti-cancer therapy as it modulates the Warburg effect in cancer cell lines.</p>

<p>Inhibitor of sodium-glucose cotransporter SGLT2</p>

<p>Inhibitor of the intracellular copper chaperones ATOX1 and CCS</p>

Gastric proton pump inhibitor

<p>Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.</p>

Pantoprazole is a proton pump inhibitor drug that is used to treat erosive esophagitis and promotes healing of tissue damage caused by gastric acid. It is used for the management of GERD. Through the proton pump inhibition, the formation of hydrochloric acid is inhibited thus inhibiting gastric secretion.

<p>A potent inhibitor of CETP that inhibits transfer of cholesteryl esters and triglycerides. Raises HDL cholesterol levels whilst lowering LDL cholesterol. Reduces cardiovascular events in patients with atherosclerotic vascular disease that receive statin treatment.</p>

<p>AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with binding affinity of 1.6 nM, 6-fold selective for MTC1 over MCT2.</p>

<p>Inhibitor of serotonin reuptake</p>

<p>Tetrabenazine is a drug that has been used for the treatment of Parkinson's disease. It acts by inhibiting dopamine release and reducing the activity of nerve cells in the brain. Tetrabenazine Bio-X is used to treat dyskinesias, that are abnormal and involuntary muscle movements by inhibiting the monoamine transporter (VMAT2).<br>Tetrabenazine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use."</p>

Dopamine reuptake inhibitor; ligand of sigma receptors

Dopamine reuptake inhibitor

<p>Serotonin uptake inhibitor; anti-depressant</p>

Venlafaxine is an antidepressant drug used in the treatment of major depression, anxiety disorder and panic disorder. It is classed as an SNRI drug meaning it inhibits the reuptake of serotonin and norepinephrine so that there is an increased level of the neurotransmitters in the synaptic cleft.

<p>A serotonin reuptake inhibitor with anticholinergic activity and mild inhibitory activity on noradrenaline reuptake. Paroxetine has been used for the treatment of depression, anxiety disorders, post-traumatic stress disorder, premenstrual dysphoric disorder and obsessive-compulsive disorder.  Also inhibits nitric oxide synthase and cytochrome isoenzyme P450 2D6.</p>

A selective inhibitor of glial glycine transporter type 1 (GlyT-1b). It has no considerable affinity for noradrenaline, dopamine, serotonin and GABA receptors. Increases amplitude of electronically evoked NMDA receptor-mediated glutamatergic excitatory postsynaptic current (eEPSCs). This raises glycine levels in spinal cord slides and extends the duration of current at glycinergic synapses.

Dapoxetine is a serotonin reuptake inhibitor drug that is used to treat premature ejaculation. This drug works by increasing the levels of serotonin in the brain, which in turn can help to delay the reflex that triggers ejaculation. As a result, it delays ejaculation and improves control over this.

<p>Imipramine is a drug that belongs to the class of tricyclic antidepressant drugs. It is used in the treatment of depression and childhood enuresis. It is a potent inhibitor of serotonin and norepinephrine reuptake. Imipramine blocks D-2 receptors, H1 receptors, α-1 and α-2 adrenergic receptors and muscarinic receptors. Also, it is indicated for dysthymia, attention-deficit disorders, agoraphobia and it is effective in treating anxiety and panic disorders.</p>

<p>Inhibitor of lactate uptake and efflux via monocarboxylate transporter MCT1. The blockade of lactate transport with BAY 8002 leads to accumulation of lactate and pyruvate in cells. The MCT1 inhibition decreased tumour growth most effectively in diffuse large B-cell lymphoma cell lines and in subsets of solid tumour models.</p>

Inhibitor of ABC transporters; oral bioenhancer for anti-cancer therapy

<p>Bupropion is an antidepressant drug that has been used in treatment trials for major depressive disorder. It has been shown to be effective in combination therapy with other drugs, such as a serotonin reuptake inhibitor (SSRI) or a tricyclic antidepressant (TCA). The drug's mechanism of action is not well understood but is said to increase the levels of dopamine and norepinephrine by inhibiting their reuptake.</p>

<p>Reboxetine mesylate is a drug that belongs to the class of tricyclic antidepressants. It is a selective and potent inhibitor of neuronal reuptake of norepinephrine (noradrenaline).  Reboxetine also interacts with neurokinin-1 receptors, which may affect locomotor activity and hippocampal formation, resulting in effects to memory and learning. It has been shown to be effective in the treatment of symptoms related to depression and Parkinson's disease.</p>

<p>Maprotiline is a tetracyclic antidepressant that is used for the treatment of major depressive disorder and anxiety that is associated with depression. This drug inhibits noradrenaline reuptake and has anticholinergic properties. Additionally, Maprotiline inhibits the amine transporter which allows for a delay in the reuptake of noradrenaline.</p>

<p>Orally available and central nervous system-penetrant inhibitor of GlyT1 glycine transporter SLC6A9. PF 03463275 was shown to enhance neuroplasticity and cognitive remediation in schizophrenia patients. In animal studies, PF 03463275 also influenced retina as changes in electroretinogram were detected in albino rats.</p>

<p>Inhibitor of CETP exchange protein</p>

<p>Inhibits protein translocation from ER to Golgi; fungal metabolite</p>

<p>Inhibitor of CETP exchange protein</p>

Specific inhibitor of the mitochondrial pyruvate carrier complexes MPC1 and MPC2. The compound blocks the pyruvate transport across the inner mitochondrial membrane and therefore reduces pyruvate influx into the gluconeogenesis. It supresses glucose production in hepatocytes and was proposed for the control of hyperglycaemia in diabetic patients. Also used for the sensitisation of cancer cell lines to chemotherapy.

<p>Dapagliflozin is a sodium-glucose cotransporter subtype 2 (SGLT2) inhibitor that can be used in the treatment of diabetes mellitus type 2. It inhibits glucose reabsorption in the proximal tubule of the nephron and results in glycosuria, which helps to improve glycaemic control. Also, Dapagliflozin is used to lower the risk of sustained eGFR decline, end-stage renal disease, cardiovascular death, and hospitalization for heart failure in patients with chronic kidney disease who are at risk of progression.</p>

<p>Fluvoxamine is a selective serotonin reuptake inhibitor that is used in the treatment of depression and obsessive-compulsive disorder. It blocks the reuptake of serotonin, enhancing its effects.</p>

Inhibitor of Na+/Ca2+ exchanger 1

<p>Potent inhibitor of the sodium-coupled citrate cotransporter SLC13A5 (NaCT, INDY). The compound is not structurally related to citrate and is selective for SLC13A over other related transporters.</p>

<p>Ezetimibe is a lipid-lowering compound that inhibits cholesterol absorption. This drug helps to lower cholesterol in primary hyperlipidemia and familial cholesterolemia. Ezetimibe targets the cholesterol transport protein Niemann-Pick C1-Like 1 (NPC1L1).</p>

<p>Amitryptylline is a tricyclic antidepressant that is used to treat depression and to relieve depression associated anxiety. Although its mechanism is not fully understood, it is suggested that this drug inhibits norepinephrine and serotonin thus increasing their concentrations at the synaptic clefts. Additionally, Amitryptylline has shown to have anticholinergic properties.</p>

<p>(S)-Citalopram oxalate or Escitalopram oxalate is the S-enantiomer of racemic Citalopram. It is a selective serotonin reuptake inhibitor that is used for the treatment of depression and anxiety disorder. Escitalopram enhances serotonergic activity by binding to the primary binding site on the serotonin transporter thus preventing the reuptake of serotonin into the presynaptic neuron.</p>

<p>Dapoxetine is a drug that belongs to the group of selective serotonin reuptake inhibitors (SSRIs). It is used to treat premature ejaculation. This drug inhibits the serotonin transporter allowing for an increased action of serotonin at the postsynaptic cleft, thus promoting ejaculatory delay.</p>

Inhibitor of ABC transporters; oral bioenhancer for anti-cancer therapy

<p>Levetiracetam is a modulates the activity of the synaptic vesicle protein 2A (SV2A) in the brain and is used to treat epilepsy.It is not clear exactly how Levetiracetam affects the activity of SV2A and if this is through inhibiting the release of neurotransmitters. However, it is thought to work by binding to a specific site on SV2A, which interferes with its normal function and ultimately leads to changes in exocytosis. One of the postulated mechanisms of action is that this modulates glutamate release. Levetiracetam is used to treat certain types of seizures in people with epilepsy.<br>Levetiracetam is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Esomeprazole is an anti-ulcer drug that is used in the treatment of GERD and to reduce the risk of ulcers associated with NSAID’s. This drug is a proton pump inhibitor that suppresses the release of gastric acid in the stomach.</p>

Sertraline is a selective serotonin reuptake inhibitor (SSRI) that is used to treat major depression, obsessive-compulsive disorder, panic disorder, posttraumatic stress disorder, and premenstrual dysphoric disorder. This drug inhibits the reuptake of serotonin which results in an increased synaptic concentration of serotonin in the CNS.

<p>Inhibitor of sodium-glucose cotransporters SGLT1 and SGLT2</p>

<p>Selective and potent inhibitor of glucose transporter GLUT1 with IC50 of 2 nM. The compound limits glucose uptake and is able to block basal as well as stress-regulated glycolysis in ovarian cancer cells. It supresses proliferation, viability and tumorigenicity of ovarian cancer cells.</p>

<p>Clomipramine is a tricyclic antidepressant drug that inhibits the reuptake of serotonin, norepinephrine, and dopamine. It is used to treat obsessive compulsive disorder, panic disorders and cataplexy. Additionally, Clomipramine is shown to modulate immune activation and shows constant anti-inflammatory properties at therapeutic concentrations by consistently decreasing pro-inflammatory cytokines.</p>

<p>Reserpine is an indole alkaloid that is found in the roots of the Rauwolfia plant. Reserpine has been shown to possess analgesic, anti-inflammatory, sedative, and anti-hypertensive properties. It is mainly used to treat mild to moderate hypertension. Reserpine inhibits the uptake of norepinephrine into storage vesicles by irreversibly blocking the vesicular monoamine transporter thus resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It is used as a pharmacological tool in research on chronic liver diseases.</p>

<p>Elacridar is an inhibitor of ATP-dependent transport, which is mediated by P-glycoprotein (P-gp). Functioning as an oral bioenhancer, Elacridar addresses multiple drug resistance in tumors, a common challenge in cancer treatment often linked to changes in the expression of protein inhibitors. Inhibition of P-gp by Elacridar is a key mechanism behind its effectiveness. P-glycoprotein, a well-characterized human ABC transporter of the MDR/TAP subfamily, acts as an ATP-dependent efflux pump with broad substrate specificity. Its increased expression in the intestines can hinder drug absorption, leading to reduced bioavailability and inadequate therapeutic plasma concentrations. Elacridar addresses this challenge by inhibiting P-gp, thereby increasing the bioavailability of coadministered drugs. Overall, Elacridar emerges as a promising option for the treatment of solid tumors, offering a strategic approach to overcoming multidrug resistance in cancer therapy.</p>

Revaprazan is a proton pump inhibitor drug that is used for the treatment of GERD and other conditions related to an excess in stomach acid production. This drug works by inhibiting the proton pump in the stomach lining known as the H+/K+-ATPase, resulting in a reduction of stomach acid and relief of symptoms.

Duloxetine is a serotonin and norepinephrine reuptake inhibitor drug that is used to treat anxiety, pain, osteoarthritis and stress incontinence. This drug inhibits the reuptake of the neurotransmitters serotonin and norepinephrine so that there are increased levels of them in the synaptic cleft.

Probenecid is a uricosuric agent that is used to treat gout and hyperuricemia. This drug works by inhibiting the reabsorption of uric acid in the renal tubes which results in more uric acid being passed out in the urine. By lowering uric acid levels, Probenecid helps prevent the formation of uric acid crystals in joints, reducing the risk of gout attacks. This drug can also be used as an adjunct to antibacterial therapy.

<p>Inhibitor of sulphonylurea receptor SUR1; hypoglycemic agent</p>

<p>Dopamine reuptake inhibitor</p>

Non-transportable inhibitor of GLT-1 glutamate transporter

Serotonin and norepinephrine reuptake inhibitor; anti-depressant

<p>P-glycoprotein (MDR1) inhibitor; non-immunosuppressive cyclosporin A analog</p>

<p>Potent P-glycoprotein (P-gp) inhibitor</p>

<p>Methyl-d3-magnesium iodide solution, 1.0 M in diethyl ether, is a specialized organometallic reagent used extensively in synthetic chemistry. This compound is a labeled Grignard reagent, where the methyl group is fully deuterated. It is sourced through the synthesis involving the reaction of deuterated methyl iodide with magnesium in an anhydrous diethyl ether solvent.</p>