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At least 19 recordsLinked to original sources
PubMed1979

Pharmacological studies on a new thymoleptic antidepressant, 1-[3-(dimethylamino)propyl]-5-methyl-3-phenyl-1H-indazole (FS-32).

Some pharmacological actions of 1-[3-(dimethylamino)propyl]-5-methyl-3-phenyl-1H-indazole (FS-32), a newly synthesized indazole derivative, were investigated in comparison with imipramine. FS-32 showed anti-reserpine activity in a dose-dependent manner, whereas imipramine exhibited a bell-shaped dose-response pattern. Catecholaminergic potentiation was demonstrated with FS-32. The results obtained from a norepinephrine potentiation test in vitro suggest that FS-32 may act in a manner qualitatively different from the tricyclic antidepressant. FS-32 produced a definite suppressive effect on isolation-induced fighting without affecting coordinated motor activity and on the duration of afterdischarge elicited by electrical stimulation to the amygdala or the hippocampus without producing a slow wave pattern in the EEG. Similar effects on fighting behavior and the afterdischarge were shown under imipramine with a slight motor incoordination and with a slow wave pattern, respectively. FS-32 produced practically no peripheral anti-cholinergic action, while it antagonized central cholinergic activity. FS-32 tended to produce an increase in chatecholamine content in the brain without MAO or COMT inhibitory activity. Norepinephrine uptake was inhibited by FS-32, but less than by imipramine. These pharmacological properties suggest a potential clinical utility of FS-32 as an antidepressant possessing thymoleptic activities.

Acetylcholine↗
PubMed1978

Effect of 1-(2,4-dichlorobenzyl)-indazole-3-carboxylic acid on sperm tails in rhesus monkeys.

Large numbers of spermatozoa with bent or coiled tails were found in the ejaculates of rhesus monkeys treated with 1-(2,4-dichlorobenzyl-indazole-3-carboxylic acid (DICA) (50 or 500 mg/kg for various periods). The defect appeared only in spermatozoa in the cauda epididymidis and consisted of axoneme disarrangement and loss of the fibre doublets. The coil was completely enclosed in a membrane.

Animals↗
PubMed1979

Characterization of the exfoliative antispermatogenic agent 1-(2,4-dichlorobenzyl)-H-indazole-3-carboxylic acid in the rhesus monkey.

The effects of oral doses of 1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxylic acid (DICA) on spermatogenesis in the rhesus monkey (Macaca mulatta) was studied. Four animals given five daily 50 mg/kg doses or three or five daily 500 mg/kg doses showed that DICA was an exfoliating antispermatogenic compound. The inhibition of spermatogenesis was only partially reversible following 500 mg/kg doses of DICA. Weekly and monthly 50 mg/kg doses of DICA only partially inhibiting spermatogenesis as measured by electro-ejaculated sperm counts. Response in individual monkeys ranged from azoospermia to no effect. Testicular biopsies confirmed this finding. DICA did not affect serum luteinizing hormone (LH), follicle-stimulating hormone (FSH), or testosterone concentrations. The blood absorption or urinary excretion rates of uniformly tritiated DICA in the animals that responded well did not differ from those monkeys that responded poorly. DICA metabolites were not detected in monkey urine. Serum testosterone concentrations appeared to vary with the season of the year, but FSH concentrations and ejaculated sperm count did not.

Animals↗
PubMed1979

1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxylic acid (DICA), an exfoliative antispermatogenic agent in the rat.

The oral administration of 50 mg DICA/kg at nine weekly or four monthly intervals produced partially reversible infertility in male rats as judged by the results of serial mating and testicular histology. Oral 500 mg DICA/kg doses administered at the same intervals produced permanent sterility. Single oral doses of 50 or 500 mg DICA/kg elevated mean FSH concentrations on days 2, 3, and 7 but did not affect LH or testosterone. Mean plasma concentration peaked at 74 micrograms/ml 4 hr after a 50 mg/kg dose of uniformly tritiated DICA; 24 hr later, it had declined rapidly to 5.5 micrograms/ml. The drug did not have a strong affinity for any tissue studied including the testis. DICA-induced exfoliation of immature germ cells was first observed 4 hr after administration and led to significantly reduced testis weights by day 2. Neither single doses of 10--250 mg DICA/kg nor five daily doses of 10--100 mg DICA/kg reduced seminal vesicle, ventral prostate, or body weights of male rats. Chronic weekly DICA administration did reduce mean seminal vesicle weight. These studies have shown that DICA is an effective, partially reversible antifertility agent that directly affects the rat testis.

Administration, Oral↗
PubMed1979

Syntheses and antiinflammatory actions of 4,5,6,7-tetrahydroindazole-5-carboxylic acids.

A novel series of 1-aryl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acids and 2-aryl-4,5,6,7-tetrahydro-2H-indazole-5-carboxylic acids were synthesized via condensation between a phenylhydrazine and a 2-(hydroxymethylene)cyclohexanone-4-carboxylate, and the antiinflammatory activity was determined. In the carrageenan edema test, 1-aryl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acids exhibited fairly high antiinflammatory activity. However, the 2-aryl isomers were far less active than the former. The most active compound of the series was 1-phenyl-4,5,6,7-tetrahydro-1H-indazole-5-carboxylic acid, which had an ED50 value of 3.5 mg/kg.

Analgesics↗
PubMed1975

Mutagenic evaluation of antischistosomal drugs and their derivatives in Neurospora crassa.

The mutagenic activities of lucanthone, hycanthone, niridazole, and the indazole analogs of lucanthone (IA-3 and IA-5) or hycanthone (IA-4 and IA-6) were studied by assaying for the induction of specific locus mutations in the ad-3 region of N. crassa. The results show that lucanthone, hycanthone, and their indazole analogs (IA-3 through IA-6) are all mutagenic in N. crassa when conidia are treated with any of these compounds. On a per mole basis, hycanthone is the least toxic and mutagenic, whereas IA-3 is the most toxic and mutagenic compound among the six closely related agents. In general, compounds with a methyl group at the C-4 position are more mutagenic than compounds with a methanol group; 6-chloroindazole analogs are more mutagenic and more toxic than nonchlorinated analogs. Niridazole is not mutagenic when conidial suspensions are treated. However, the mutation frequency increased more than 50-fold when niridazole was added to the medium used to grow vegetative cultures. Thus, it appears that the mutagenic activity of this latter compound requires metabolic activation.

Hycanthone↗
PubMed1978

Mutagenicity of some commercially available nitro compounds for Salmonella typhimurium.

Benzoyl chloride and 53 commercially available aromatic heterocyclic and aliphatic nitro compounds were tested for mutagenicity in Salmonella typhimurium TA98 and TA100. 34 of 53 nitro compounds (64%) were mutagenic, 4 in TA100 only, 15 in TA98 only, and 15 in both strains. 13 of the heterocyclic derivatives of pyridine, indole, indazole, quinoline, and benzimidazole were mutagenic. 21 of 34 mutagenic nitro compounds were bactericidal. Nitromethane was the only aliphatic tested and was not mutagenic. Benzoyl chloride, a human carcinogen, was mutagenic for TA98.

Anti-Bacterial Agents↗
PubMed1979

Induction of hepatic neoplastic lesions in mice with a single dose of hycanthone methanesulfonate after partial hepatectomy.

Experiments were designed to determine whether hycanthone methanesulfonate (1-([2-(diethylamino)ethyl]amino)-4-(hydroxymethyl)thioxanthen-9-one monomethanesulfonate), an antischistosomal drug, and its analog, IA-4-N-oxide (8-chloro-2-[2-(diethylamino)ethyl]-2H-[1]benzothiopyrano[4,3,2-cd]indazole 5-methanol monomethanesulfonate), will induce neoplastic lesions in the livers of mice not infected with Schistosoma mansoni. All the mice received a single i.m. injection of hycanthone methanesulfonate (76 mg/kg), IA-4-N-oxide (80 mg/kg), or an equivalent volume of the solvent, 0.9% NaCl solution, 42 hr after partial hepatectomy. Of the mice receiving hycanthone methanesulfonate and living 200 days or longer, hepatocellular carcinoma was seen in 11.5% and liver sarcoma was seen in 4.2%. This type of malignant neoplasm was not seen in the animals receiving either IA-4-N-oxide or 0.9% NaCl solution. In addition, mice receiving hycanthone methanesulfonate showed a significantly higher incidence of both type 1 (43% compared to 21% in controls) and type 2 (21% compared to 12% in controls) hepatocyte neoplasms. Mice receiving IA-4-N-oxide showed no increased incidence of neoplasms.

Animals↗
PubMed2026

The Long Road to Long-Acting: What Oral PrEP and CAB-LA Teach Us About Scaling Lenacapavir.

Despite significant biomedical advances, human immunodeficiency virus (HIV) remains a persistent global health crisis, with over 40 million people affected as of 2023, two-thirds of whom live in the World Health Organization (WHO) African Region. However, from an HIV prevention perspective, the more urgent concern is the continued occurrence of approximately 1.3 million new infections annually, particularly in sub-Saharan Africa and in settings where incidence is stable or increasing. This commentary explores the evolving landscape of HIV prevention, focusing on the trajectory of oral pre-exposure prophylaxis (PrEP), long-acting injectable cabotegravir (CAB-LA), and the newly emerging lenacapavir. While oral PrEP opened new possibilities, adherence challenges have limited its impact. CAB-LA demonstrated superior efficacy but encountered access, cost, and delivery barriers that restricted uptake. Lenacapavir, offering 6-monthly subcutaneous dosing with ≥ 99.9% efficacy in trials, holds the potential to overcome these hurdles. As of May 2026, lenacapavir had received regulatory approval in 17 countries, including several African nations, while regulatory reviews remained ongoing in multiple additional countries, reflecting the rapid global expansion of access to this long-acting HIV prevention option. However, its success depends on clinical promise, timely licensing, affordability, and integration into health systems. Drawing from real-world lessons of oral PrEP and CAB-LA, this paper argues that a proactive, coordinated rollout of lenacapavir could dramatically expand prevention reach. With global stakeholders aiming for 3 million users by 2028 and strategic licensing in 120 countries, the groundwork is in place. The recent release of WHO guidance recommending lenacapavir as an additional PrEP option further strengthens this momentum. Yet, equitable delivery, user-centred models, and strong policy backing will be critical. Ultimately, long-acting PrEP is not just a clinical breakthrough; it is a test of health systems' ability to deliver innovation at scale.

Humans↗