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    • Paul A J Janssen
    • Paul A J Janssen

      Paul A J Janssen

      Division of Pharmacology, Research Department, Laboratoria Pharmaceutica, Dr. C. Janssen, Beerse, Belgium | From Janssen Pharmaceutica, N.V., Research Laboratoria, Beerse ...



      KOL Resume for Paul A J Janssen


      Division of Pharmacology, Research Department, Laboratoria Pharmaceutica, Dr. C. Janssen, Beerse, Belgium


      Research Laboratories, Janssen Pharmaceutica, B‐2340 Beerse, Belgium


      Center for Advanced Biotechnology and Medicine and Department of Chemistry and Chemical Biology, Rutgers University, 679 Hoes Lane, Piscataway, New Jersey 08854, Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry, 675 Hoes Lane, Piscataway, New Jersey 08854, and Center for Molecular Design, Janssen Pharmaceutica NV, Antwerpsesteenweg, 37, B2350 Vosselaar, Belgium


      Center for Molecular Design, Janssen Pharmaceutica, Vosselaar Belgium


      Center for Molecular Design, Johnson & Johnson Pharmaceutical Research and Development, Janssen Pharmaceutica N.V., Antwerpsesteenweg 37, 2350 Vosselaar, Belgium


      Center for Molecular Design, Janssen Pharmaceutica N.Y., Belgium


      Center for Molecular Design, Antwerpsesteenweg 37, Vosselaar, Belgium, BE


      Centre for Molecular Design, Janssen Research Foundation, B-2340 Beerse, Belgium


      Department of Chemistry, Western Maryland College, Westminster, Maryland 21157, ABL-Basic Research Program, NCI−Frederick Research and Development Center, P.O. Box B, Frederick, Maryland 21702-1201, Department of Chemistry, Yale University, New Haven, Connecticut 06520-8107, and Janssen Research Foundation, CMD, Antwerpsesteenweg 37, B-2350 Vosselaar, Belgium


      Janssen Research Foundation B‐2340 Beerse, Belgium


      ABL-Basic Research Program, NCI-Frederick Cancer Research and Development Center, P.O. Box B, Frederick, MD 21701-1013, USA

      TIBOTEC, Institute for Antiviral Research, Drie Eikenstraat 661, B-2650 Edegem, Belgium


      Janssen Research Foundation, Turnhoutseweg 30, B-2340, Beerse, Belgium

      Center for Advanced Biotechnology and Medicine (CABM) and Rutgers University Chemistry Department, 679 Hoes Lane, 08854-5638, Piscataway, New Jersey, USA


      Janssen Research Foundation, Beerse, Belgium.


      Janssen Research Foundation, B-2340, Beerse, Belgium


      Janssen Research Foundation, Beerse, Belgium *Department of Medicine, Prince of Wales Hospital, Chinese University of Hong Kong, Hong Kong


      From the Janssen Research Foundation

      Janssen Pharmaceutica, Beerse, Belgium


      Department of Neuropsychopharmacology, Janssen Research Foundation, Beerse Belgium


      Department of Biochemistry, Janssen Pharmaceutica, Beerse, Belgium

      From the Janssen Research Foundation, Beerse

      Janssen Research Foundation, Spring House, PA, U.S.A.


      Department of Biochemical pharmacology, Janssen Research Foundation, B-2340, Beerse, Belgium



      Paul A J Janssen: Influence Statistics

      Sample of concepts for which Paul A J Janssen is among the top experts in the world.
      Concept World rank
      heterogenous chemical structure #1
      pimozideprotein conjugate pimozide #1
      astemizole mequitazine #1
      drugs trifluperidol #1
      ketanserin reaction #1
      ritanserin pirenperone #1
      moperone #1
      trifluperidol animals #1
      role serotonin release #1
      intraperitoneal male saperconazole #1
      animal models activity #1
      castration castrated animals #1
      r82913 hiv1 #1
      saline 2lever procedure #1
      alfentanil eeg measures #1
      physiology sleepwakefulness regulation #1
      nalorphine nallylnormetazocine #1
      prostanoids ridogrel #1
      class calcium antagonist #1
      setoperone ritanserin #1
      astemizole ascaris #1
      percentage discrimination #1
      profile nebivolol #1
      dextromoramide fentanyl humans #1
      noberastine #1
      constant 1 infusion #1
      cardiac cells effects #1
      ketanserin 20 #1
      abstract5hydroxytryptamine serotonin #1
      rats shuttle box #1
      potent antagonist clonidine #1
      terfenadine oral activity #1
      astemizole antihistamines #1
      rat liver drugconcentrations #1
      dlnebivolol ventricular function #1
      txa2 molecule #1
      lsdcue #1
      sr3nebivolol #1
      ketotifen slowwave sleep #1
      dilute tissue suspensions #1
      prostaglandin biosynthesis evolution #1
      tumour grafts combination #1
      pca reactions inhibition #1
      chronic treatment setoperone #1
      pirenperone response #1
      ketanserin prototype #1
      mast cells astemizole #1
      setoperone dopamine #1
      influence haloperidol #1
      β‐adrenergic blocking agents #1


      Prominent publications by Paul A J Janssen

      KOL-Index: 17313

      Human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) is an important target for chemotherapeutic agents used in the treatment of AIDS; the TIBO compounds are potent non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Crystal structures of HIV-1 RT complexed with 8-Cl TIBO (R86183, IC50 = 4.6 nM) and 9-Cl TIBO (R82913, IC50 = 33 nM) have been determined at 3.0 A resolution. Mutant HIV-1 RT, containing Cys in place of Tyr at position 181 (Tyrl81Cys), is highly resistant to ...

      Known for Crystal Structures | Type Hiv1 | P66 Subunit | 8cl Tibo | Xray Drug Resistance
      KOL-Index: 16345

      Ritanserin is a potent and selective serotonin-S2 antagonist which slowly dissociates from the receptor sites, while setoperone has potent serotonin and moderate dopamine antagonistic properties and dissociates rapidly from the receptor sites. Acute administration of ritanserin (1–10 mg/kg) produced a non-competitive inhibition of 3H-ketanserin binding, measured ex vivo in washed frontal cortex membranes, which lasted for 12 h. This is in accordance with the slow dissociation of the drug ...

      Known for Receptor Sites | Rat Brain | Chronic Treatment | Bmax Values | Serotonin Ritanserin
      KOL-Index: 11238

      Recently developed agents specifically acting on different 5-hydroxytryptamine (5-HT) receptor populations were used to analyze the functional role of 5-HT2 receptor subtypes in the sleep-wakefulness cycle of the rat. The 5-HT2 receptor antagonist ritanserin injected intraperitoneally (IP) (0.04–2.5 mg/kg) induced an increase in deep slow wave sleep (SWS2) duration at the expense of wakefulness (W), light slow wave sleep (SWS1) and paradoxical sleep (PS). The stimulation of 5-HT2 ...

      Known for Ht2 Receptors | Functional Role | Sleep Wakefulness | Increase Sws1 | 8 Hydroxy2di
      KOL-Index: 11227

      This study determined the limits of discriminability of cocaine HCl and the role of the training dose of cocaine in cocaine-saline discrimination. Rats were trained to discriminate 10 mg/kg of cocaine HCl from saline in a two-lever operant procedure, and then were retrained on progressively smaller doses of the training drug. Stimulus generalization experiments with test doses of cocaine 12 to 1250 times the training dose, were carried out each time the animals had reached criterion on ...

      Known for Training Dose | Effects Cocaine | Discrimination Rats | Stimulus Generalization | Drug Saline
      KOL-Index: 10992

      The experiments reported here were undertaken to examine the neuropharmacological characteristics of drugs inducing stimulus generalization with cocaine as a cue. Experiment 1 indicated that d-amphetamine (ED50: 0.17 mg/kg), 1-amphetamine (0.45 mg/kg), methylamphetamine (0.15 mg/kg), methylphenidate (0.55 mg/kg) and nomifensine (0.32 mg/kg) induce stimulus generalization with cocaine in rats trained to discriminate 10 mg/kg cocaine from saline; this generalization occurred in 100% of the ...

      Known for Stimulus Generalization | Cocaine Rats | Adrenergic Beta | Discrimination Psychological | Trained Discriminate
      KOL-Index: 10704

      Ketanserin, a selective 5-HT2-receptor antagonist, inhibits the reversible aggregation induced by 5-hydroxytryptamine (5-HT) in human platelet-rich plasma (PRP). In this respect, the compound is equipotent to cyproheptadine and more active than methysergide (IC50: 1.66×10−8M, 1.44×10−8M and 5.62×10−8M respectively). Ketanserin is active against 5-HT-induced platelet aggregation after bothin vitro and oral administration to human volunteers. At concentrations up to 500 times in excess of ...

      Known for Human Platelet | Receptor Antagonist | Selective 5 | Oral Administration | Aggregation Induced
      KOL-Index: 10588

      Monte Carlo (MC) simulations in combination with a linear response approach were used to estimate the free energies of binding for a series of 12 TIBO nonnucleoside inhibitors of HIV-1 reverse transcriptase. Separate correlations were made for the R6 and S6 absolute conformations of the inhibitors, as well as for the analogous N6-monoprotonated species. Models based upon the neutral unbound inhibitors produced overall better fits to experimental values than did those using the protonated ...

      Known for Tibo Inhibitors | Linear Response Method | Binding Affinities | Carlo Simulations | Reverse Transcriptase
      KOL-Index: 10416

      The effects of four reference antihistamines: ketotifen, diphenhydramine, chlorpheniramine and pyrilamine and of astemizole, a new potent and long-acting antihistamine, were studied on 16 hr sleep-wakefulness patterns in the same dogs. Using a computer-based on-line analysis and automatic stage classification, a differentiation was made between wakefulness, transition to sleep (drowsiness), slow wave sleep and rapid eye movement (REM) sleep. The reference antihistamines significantly ...

      Known for Rem Sleep | Antihistamines Astemizole | Brain Histamine | H1 Receptors | Dogs Effects
      KOL-Index: 10368

      Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are potent inhibitors of human immunodeficiency virus type 1 (HIV-1); however, currently marketed NNRTIs rapidly select resistant virus, and cross-resistance within the class is extensive. A parallel screening strategy was applied to test candidates from a series of diarylpyrimidines against wild-type and resistant HIV strains carrying clinically relevant mutations. Serum protein binding and metabolic stability were addressed early ...

      Known for Virus Type | Reverse Transcriptase | Resistant Human | Preclinical Drug Resistance | Generation Nonnucleoside

      Key People For Neuroleptic Drugs

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      Paul A J Janssen:Expert Impact

      Concepts for whichPaul A J Janssenhas direct influence:Neuroleptic drugs,  Stimulus generalization.

      Paul A J Janssen:KOL impact

      Concepts related to the work of other authors for whichfor which Paul A J Janssen has influence:Reverse transcriptase,  Dopamine receptors,  Blood pressure,  Animal models,  5 ht,  Antipsychotic drugs,  Nucleus accumbens.



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      Division of Pharmacology, Research Department, Laboratoria Pharmaceutica, Dr. C. Janssen, Beerse, Belgium | From Janssen Pharmaceutica, N.V., Research Laboratoria, Beerse (Belgium). | Department of Pharmacology, Janssen Pharmaceutica Research Laborat

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