first-generation

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Antazoline hydrochloride (Phenazoline hydrochloride), a first-generation antihistamine, can bind to the histamine H1 receptor and block the action of endogenous histamine.

Cephalonium (Cefalonium) is a first-generation cephalosporin antibiotic.

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity, exhibiting greater binding affinity to SUR1 and increased potency compared to first-generation compounds. Additionally, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Promethazine hydrochloride (Promethazine HCl) , the first-generation antihistamine, is a strong antagonist of the H1 receptor and a moderate antagonist of the mACh receptor, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

Cefazolin sodium (cephazolin sodium) salt binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cefazolin sodium salt is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

6-Benzylaminopurine (6-BAP), benzyl adenine or BAP is a first-generation synthetic cytokinin that elicits plant growth and development responses, setting blossoms and stimulating fruit richness by stimulating cell division. It is an inhibitor of respiratory kinase in plants, and increases post-harvest life of green vegetables.

Cephalothin sodium (Cefalotin) binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cephalothin sodium (Cefalotin) is the sodium salt form of cephalothin, a semisynthetic, beta-lactam, the first-generation cephalosporin antibiotic with bactericidal activity. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Fexofenadine (Carboxyterfenadine), an antihistamine pharmaceutical drug, is used to treat allergy symptoms, such as nasal congestion, hay fever, and urticaria. Compared to first-generation antihistamines, Fexofenadine is less able to pass the blood-brain barrier and cause sedation.

Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.

Etravirine (R165335) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT.

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

Cephapirin Benzathine is a semisynthetic, broad-spectrum, first-generation cephalosporin with antibacterial activity.

Imipramine hydrochloride (Imipramine HCl) is a first generation tricyclic antidepressant that acts primarily as an inhibitor of serotonin and norepinephrine transporters (Kds = 1.4 and 37 nM, respectively).Imipramine hydrochloride is reported to prevent the translocation of aSMase, inhibiting MV and exosomes secretion

Diphenylpyraline hydrochloride (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) is used in the treatment of Parkinsonism.It is a first-generation antihistamine with anticholinergic effects, functions as a dopamine reuptake inhibitor.

Diphenylpyridine is the first generation antihistamine, which has the anticholinergic effect of diphenylpiperidine.

Cefalonium Dihydrate(5575-21-3 free base) is a first-generation cephalosporin antibiotic.

Cephradine (Anspor) is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.

Cefadroxil is a first generation aminocephalosporin with good patient compliance, a long-acting therapeutic effect, high solubility and relatively broad spectrum of anti-bacterial activity. Cefadroxil is also a substrate of the intestinal peptide transporter PepT1, which is primarily responsible for the drug's uptake across the apical membrane of small intestine.

Promethazine is a neuroleptic medication and first-generation antihistamine of the phenothiazine family.

Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.

Cephradine monohydrate, a first-generation cephalosporin, is active against a wide range of Gram-positive and Gram-negative bacteria.