Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, binding with small molecules in extracellular space, the recognition process in the immune system, energy transduction, osmoregulation, and physiological and developmental processes. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters.

ATP-powered pumps are ATPases that use the energy of ATP hydrolysis to move ions or small molecules across a membrane against a chemical concentration gradient or electric potential. Channel proteins transport water or specific types of ions down their concentration or electric potential gradients. Many other types of channel proteins are usually closed, and open only in response to specific signals. Because these types of ion channels play a fundamental role in the functioning of nerve cells. Transporters, a third class of membrane transport proteins, move a wide variety of ions and molecules across cell membranes. Membrane transporters either enhance or restrict drug distribution to the target organs. Depending on their main function, these membrane transporters are divided into two categories: the efflux (export) and the influx (uptake) transporters.

Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system ion channels have been linked to many diseases such, but not limited to, ataxias, paralyses, epilepsies, and deafness indicative of the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Furthermore, drug transporters can serve as drug targets or as a mechanism to facilitate drug delivery to cells and tissues.

References:
[1] Sadée W, et al. Pharm Res. 1995 Dec;12(12):1823-37.
[2] Girardin F. Dialogues Clin Neurosci. 2006;8(3):311-21.
[3] Zaydman MA, et al. Chem Rev. 2012 Dec 12;112(12):6319-33.
[4] Mishra NK, et al. PLoS One. 2014 Jun 26;9(6):e100278.


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Manidipine

Manidipine is a calcium channel blocker that is used clinically as an antihypertensive. Target: Calcium ChannelManidipine is a dihydropyridine calcium antagonist, which causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine was well tolerated in clinical trials, with most adverse effects related to vasodilation [1]. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. manidipine represents a first-line treatment option for patients with essential mild-to-moderate hypertension [2]. Manidipine has neutral effects on glucose and lipid metabolism and is generally well tolerated. Manidipine thus represents a first-line option for lowering BP in patients with mild-to-moderate hypertension [3].

  • CAS Number: 89226-50-6
  • MF: C35H38N4O6
  • MW: 610.699
  • Catalog: Calcium Channel
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 722.0±60.0 °C at 760 mmHg
  • Melting Point: 125-128ºC
  • Flash Point: 390.4±32.9 °C

Arecaidine hydrochloride

Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].

  • CAS Number: 6018-28-6
  • MF: C7H12ClNO2
  • MW: 177.62900
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 266.7ºC at 760 mmHg
  • Melting Point: 260ºC
  • Flash Point: 115.1ºC

H-Phe-Met-Arg-Phe-NH2 acetate salt

Phe-Met-Arg-Phe, amide acetate dose dependently (ED50=23 nM) activates a K+ current in the peptidergic caudodorsal neurons[1].

  • CAS Number: 152165-14-5
  • MF: C31H46N8O6S
  • MW: 658.81
  • Catalog: Potassium Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cytisine

Cytisine is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisine is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. has been used medically to help with smoking cessation[3].

  • CAS Number: 485-35-8
  • MF: C11H14N2O
  • MW: 190.242
  • Catalog: nAChR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 413.0±34.0 °C at 760 mmHg
  • Melting Point: 154-156ºC
  • Flash Point: 203.6±25.7 °C

DDO-02005 free base

DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine[1].

  • CAS Number: 1186134-30-4
  • MF: C21H25N3O2
  • MW: 351.44
  • Catalog: Potassium Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bulleyaconitine A

Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.

  • CAS Number: 107668-79-1
  • MF: C35H49NO9
  • MW: 627.765
  • Catalog: Sodium Channel
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 690.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 371.7±31.5 °C

borneol

DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. DL-Borneol is widely used for the treatment of cardiovascular and cerebrovascular diseases in China.

  • CAS Number: 507-70-0
  • MF: C10H18O
  • MW: 154.249
  • Catalog: GABA Receptor
  • Density: 1.011
  • Boiling Point: 212.0±0.0 °C at 760 mmHg
  • Melting Point: 206-207ºC
  • Flash Point: 65 ºC

SGLT1/2-IN-1

SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor extract from WO2015032272A1, compound 2 [1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KB-R7943 mesylate

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM.

  • CAS Number: 182004-65-5
  • MF: C17H21N3O6S2
  • MW: 427.495
  • Catalog: Na+/Ca2+ Exchanger
  • Density: N/A
  • Boiling Point: 534.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 277.1ºC

TAT-GluA2 3Y

TAT-GluA2 3Y is an inhibitor of AMPA receptor endocytosis. TAT-GluA2 3Y induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. TAT-GluA2 3Y also exhibits antinociceptive effects in a rat model of neuropathic pain. TAT-GluA2 3Y rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.

  • CAS Number: 1404188-93-7
  • MF: C115H185N43O29
  • MW: 2634.02
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ifenprodil tartrate

Ifenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.

  • CAS Number: 23210-58-4
  • MF: C21H27NO2.1/2C4H6O6
  • MW: 400.49
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: 493.5ºC at 760mmHg
  • Melting Point: 178-180ºC
  • Flash Point: 248.7ºC

AR-C155858

AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.

  • CAS Number: 496791-37-8
  • MF: C21H27N5O5S
  • MW: 461.535
  • Catalog: Monocarboxylate Transporter
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 763.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 415.3±35.7 °C

Perzinfotel

Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site[1][2].

  • CAS Number: 144912-63-0
  • MF: C9H13N2O5P
  • MW: 260.18400
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Choline-13C2 chloride

Choline-13C2 (chloride) is the 13C labeled Choline chloride[1]. Choline chloride is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders[2][3].

  • CAS Number: 202190-49-6
  • MF: C313C2H14ClNO
  • MW: 141.61
  • Catalog: nAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ethapon

2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4)[1].

  • CAS Number: 115-20-8
  • MF: C2H3Cl3O
  • MW: 149.404
  • Catalog: Potassium Channel
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 152.1±35.0 °C at 760 mmHg
  • Melting Point: 17.8 °C(lit.)
  • Flash Point: 45.8±25.9 °C

P2X7 receptor antagonist-3

P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats[1].

  • CAS Number: 1627900-92-8
  • MF: C17H12ClF3N6O
  • MW: 408.76
  • Catalog: P2X Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isradipine-d3

Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].

  • CAS Number: 1189959-59-8
  • MF: C19H18D3N3O5
  • MW: 374.40600
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THDOC

3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

  • CAS Number: 567-02-2
  • MF: C21H34O3
  • MW: 334.49300
  • Catalog: GABA Receptor
  • Density: 1.115g/cm3
  • Boiling Point: 470.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 252.3ºC

Arecaidine

Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].

  • CAS Number: 499-04-7
  • MF: C7H11NO2
  • MW: 141.168
  • Catalog: GABA Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 266.7±35.0 °C at 760 mmHg
  • Melting Point: 232ºC (dec.)
  • Flash Point: 115.1±25.9 °C

OptoBI-1

OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing[1].

  • CAS Number: 2415272-11-4
  • MF: C32H37N5O2
  • MW: 523.67
  • Catalog: TRP Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Halofantrine

Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum[1]. Halofantrine blocks HERG potassium channels[2].

  • CAS Number: 69756-53-2
  • MF: C26H30Cl2F3NO
  • MW: 500.42400
  • Catalog: Potassium Channel
  • Density: 1.244 g/cm3
  • Boiling Point: 596.2ºC at 760 mmHg
  • Melting Point: 136-138ºC
  • Flash Point: 314.4ºC

VK-II-36

VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca2+release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations[1].

  • CAS Number: 955371-66-1
  • MF: C26H26N2O5
  • MW: 446.50
  • Catalog: Calcium Channel
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 698.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 376.3±31.5 °C

Cloperastine fendizoate

Cloperastine fendizoate inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.

  • CAS Number: 85187-37-7
  • MF: C40H38ClNO5
  • MW: 648.186
  • Catalog: Potassium Channel
  • Density: N/A
  • Boiling Point: 593.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 327ºC

Zosuquidar trihydrochloride

Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.

  • CAS Number: 167465-36-3
  • MF: C32H34Cl3F2N3O2
  • MW: 636.987
  • Catalog: P-glycoprotein
  • Density: N/A
  • Boiling Point: 690.5ºC at 760mmHg
  • Melting Point: 172-176°C
  • Flash Point: 371.4ºC

Di(N-desethyl) Amiodarone Hydrochloride

Di-N-desethyl Amiodarone hydrochloride is a metabolite of Amiodarone (HY-14187). Di-N-desethyl Amiodarone hydrochloride is a strong inhibitor of the respiratory chain[1].

  • CAS Number: 757220-04-5
  • MF: C21H22ClI2NO3
  • MW: 625.67
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Epiboxidine hydrochloride

Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418[1].

  • CAS Number: 862909-67-9
  • MF: C10H15ClN2O
  • MW: 214.69
  • Catalog: nAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

κM-Conotoxin RIIIK

κM-Conotoxin RIIIK is a potassium channel antagonist. κM-Conotoxin RIIIKcan block voltage-activated potassium ion channels [1].

  • CAS Number: 740843-55-4
  • MF: C106H178N34O33S6
  • MW: 2649.15
  • Catalog: Potassium Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Endovion

Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor[1][2].

  • CAS Number: 265646-85-3
  • MF: C16H9BrF6N6O
  • MW: 495.18
  • Catalog: Chloride Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CP-465022 Maleate

CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].

  • CAS Number: 199656-46-7
  • MF: C30H28ClFN4O5
  • MW: 579.02
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Phenylalanine-3-13C

L-Phenylalanine-3-13C ((S)-2-Amino-3-phenylpropionic acid-3-13C) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].

  • CAS Number: 136056-02-5
  • MF: C813CH11NO2
  • MW: 166.18200
  • Catalog: Calcium Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 270-275ºC (dec.)(lit.)
  • Flash Point: N/A