pharmacologically

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

BTSA1 is a BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.

(±) Clopidogrel hydrogen sulfate (Iscover) , an antiplatelet agent pharmacologically and structurally analogous to ticlopidine, is used to inhibit blood clots in various conditions such as cerebrovascular disease, peripheral vascular disease, and coronary artery disease.

Dexchlorpheniramine Maleate (S-(+)-Chlorpheniramine maleate salt) is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It is the pharmacologically active dextrorotatory isomer of chlorpheniramine.

Fenclonine (CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine(CP-10188) acts pharmacologically to deplete endogenous levels of serotonin.

Levamlodipine (S-amlodipine) belongs to the dihydropyridine group of calcium channel blockers. Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.

Articaine hydrochloride (Hoe-045), a thiophene-containing local anesthetic, is pharmacologically similar to mepivacaine.

Levamlodipine besylate ((S)-Amlodipine Besylate (103129-82-4(free base))) , also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. Levamlodipine besylate belongs to the dihydropyridine group of calcium channel blockers. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.

Hydroxyhexamide ((±)-Hydroxyhexamid) is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agent.

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

Fluvoxamine (DU-23000) is a selective, orally available 5-HT and serotonin reuptake inhibitor (SSRI) exhibiting antidepressant effects.

N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.

Tocainide hydrochloride, a sodium channel blocker, inhibits the sodium channels in the pain-producing foci in nerve membranes. It is an orally effective antiarrhythmic agent, structurally and pharmacologically similar to lidocaine [1][2].

GP531 is a second-generation adenosine regulating agent. It is pharmacologically silent under basal conditions but increases localized endogenous adenosine during ischemia.

Naproxen is a COX-1 and COX-2 inhibitor (IC50s: 8.72 and 5.15 μM, respectively in cell assay). Naproxen etemesil is a lipophilic and non-acidic prodrug of naproxen. It is hydrolyzed to pharmacologically active Naproxen once absorbed.

Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver, assisting BOS pharmacologically with 10%-20% activity retention.

Eptaloprost is a novel PGI2 analogue, designed to be converted into the pharmacologically active cicaprost through a process of β-oxidation.

Theophylline ephedrine is a pharmacologically active salt used for the treatment of obstructive ventilatory disorders.

Pirlindole, a reversible inhibitor of monoamine oxidase A (RIMA), has been developed and used primarily as an antidepressant compound in Russia. Structurally and pharmacologically, it is similar to metralindole. Pirlindole has received approval for the treatment of depression in several European and non-European countries. Its oral absolute bioavailability ranges from 20% to 30%, mainly due to significant first-pass metabolism. In rats, the oral Tmax varies between 2.5 and 6 hours, while in dogs, it ranges from 0.8 to 2 hours.

Pirlindole, a reversible inhibitor of monoamine oxidase A (RIMA), was developed and is used as an antidepressant in Russia. It is structurally and pharmacologically related to metralindole. Pirlindole has been approved for the treatment of depression in several European and non-European countries. Due to extensive first-pass effects, its absolute bioavailability ranges from 20% to 30%. When administered orally, the Tmax in rats varies from 2.5 to 6 hours, while in dogs it ranges from 0.8 to 2 hours.

Quinapril is an orally active, non-peptide, and non-thiol angiotensin-converting enzyme (ACE) inhibitor. It primarily blocks the conversion of angiotensin I to angiotensin II in both plasma and tissues. Upon enzymatic hydrolysis, Quinapril is converted into the pharmacologically active Quinaprilat and is effective in hypertension models.

Lu 25-077 is a pharmacologically active N-demethylated metabolite of Lu 25-109 that can penetrate the blood-brain barrier. Lu 25-109 functions as a partial M1 agonist and an M2/M3 antagonist. Lu 25-077 is applicable in neuroscience research.

3-Ethylquinoline is a heterocyclic aromatic biomedical compound, specifically a quinoline derivative with an ethyl substituent at the 3-position, which is utilized in various research applications, often as a synthetic intermediate or a structural motif in the development of pharmacologically active molecules.

Levolansoprazole ((S)-Lansoprazole), a proton pump inhibitor, irreversibly inhibits H+/K+-stimulated ATPase pumps in parietal cells (IC50: 5.2 μM). It also inhibits acid formation in isolated canine parietal cells (IC50: 82 μM). Both (R)- and (S)-lansoprazole are pharmacologically active with similar potencies.