Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers (516 views)
Molecules (ISSN: 1420-3049, 1420-3049electronic, 1420-3049linking), 2010 Jul 15; 15(7): 4924-4933.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 1.988, 5-year impact factor: 1.974
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-77954975254&partnerID=40&md5=6cf34d0eb54b088d9c1fd7bf925922c3
Keywords: Solid-Phase, Trp(nps) Dipeptides, Trpv1 Channel Blockers, Alkane, Guanidine, Lysine, Trpv1 Protein, Human, Tryptophan, Vanilloid Receptor, Article, Drug Antagonism, Structure Activity Relation, Synthesis, Structure-Activity Relationship, Trpv Cation Channels, Trp (nps) Dipeptides,
Affiliations:
*** IBB - CNR ***
Instituto de Química Médica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain
Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain
IBMC-UMH, Ed. Torregaitán, Av. de la Universidad s/n, 03202 Elche, Spain
Instituto de Qu mica M dica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
References:
Levine, J.D., Alessandri-Haber, N., TRP channels: Targets for the relief of pain (2007) Biochim. Biophys. Acta, 1772, pp. 989-100
Planells-Cases, R., Garcìa-Sanz, N., Morenilla-Palao, C., Ferrer-Montiel, A., Functional aspects and mechanisms of TRPV1 involvement in neurogenic inflammation that leads to thermal hyperalgesia (2005) Pflugers Arch., 451, pp. 151-159
Gunthorpe, M.J., Chizh, B.A., Clinical development of TRPV1 antagonists: Targeting a pivotal point in the pain pathway (2009) Drug Discov. Today, 14, pp. 56-67
Patapoutian, A., Tate, S., Woolf, C.J., Transient receptor potential channels: Targeting pain at the source (2009) Nat. Rev. Drug Discov., 8, pp. 55-68
García-Martínez, C., Morenilla-Palao, C., Planells-Cases, R., Merino, J.M., Ferrer-Montiel, A., Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties (2000) J. Biol. Chem., 275, pp. 32552-32558
García-López, M.T., Herranz, R., González-Muñiz, R., Naranjo, J.R., De Ceballos, M., Del Río, J., Antinociceptive effects in rodents of the dipeptide Lys-Trp(Nps) and related compounds (1986) Peptides, 7, pp. 39-43
Bonache, M.A., García-Martínez, C., García De Diego, L., Carreno, C., Pérez De Vega, M.J., García-López, M.T., Ferrer-Montiel, A., González-Muñiz, R., Old molecule for new receptors: Trp(Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
Szardenings, A.K., Burtoth, T.S., Look, G.C., Campbell, D.A.A., Reductive alkylation procedure applicable to both solution- and solid-phase syntheses of secondary amines (1996) J. Org. Chem., 61, pp. 6720-6722
Shey, J.-Y., Sun, C.-M., Soluble polymer supported synthesis of N,N-di(Boc)-protected guanidines (1998) Synlett, pp. 1423-1425
Del Fresno, M., El-Faham, A., Carpino, L.A., Royo, M., Albericio, F., Substituted guanidines: Introducing diversity in combinatorial chemistry (2000) Org. Lett., 2, pp. 3539-3542
Farrera-Sinfreu, J., Royo, M., Albericio, F., Undesired removal of the Fmoc group by the free ε-amino function of a lysine residue (2002) Tetrahedron Lett., 43, pp. 7813-7815
Levine, J. D., Alessandri-Haber, N., TRP channels: Targets for the relief of pain (2007) Biochim. Biophys. Acta, 1772, pp. 989-100
Gunthorpe, M. J., Chizh, B. A., Clinical development of TRPV1 antagonists: Targeting a pivotal point in the pain pathway (2009) Drug Discov. Today, 14, pp. 56-67
Garc a-Mart nez, C., Morenilla-Palao, C., Planells-Cases, R., Merino, J. M., Ferrer-Montiel, A., Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties (2000) J. Biol. Chem., 275, pp. 32552-32558
Garc a-L pez, M. T., Herranz, R., Gonz lez-Mu iz, R., Naranjo, J. R., De Ceballos, M., Del R o, J., Antinociceptive effects in rodents of the dipeptide Lys-Trp (Nps) and related compounds (1986) Peptides, 7, pp. 39-43
Bonache, M. A., Garc a-Mart nez, C., Garc a De Diego, L., Carreno, C., P rez De Vega, M. J., Garc a-L pez, M. T., Ferrer-Montiel, A., Gonz lez-Mu iz, R., Old molecule for new receptors: Trp (Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
Szardenings, A. K., Burtoth, T. S., Look, G. C., Campbell, D. A. A., Reductive alkylation procedure applicable to both solution- and solid-phase syntheses of secondary amines (1996) J. Org. Chem., 61, pp. 6720-6722
Shey, J. -Y., Sun, C. -M., Soluble polymer supported synthesis of N, N-di (Boc) -protected guanidines (1998) Synlett, pp. 1423-1425
Molecules (ISSN: 1420-3049, 1420-3049electronic, 1420-3049linking), 2010 Jul 15; 15(7): 4924-4933.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 1.988, 5-year impact factor: 1.974
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-77954975254&partnerID=40&md5=6cf34d0eb54b088d9c1fd7bf925922c3
Keywords: Solid-Phase, Trp(nps) Dipeptides, Trpv1 Channel Blockers, Alkane, Guanidine, Lysine, Trpv1 Protein, Human, Tryptophan, Vanilloid Receptor, Article, Drug Antagonism, Structure Activity Relation, Synthesis, Structure-Activity Relationship, Trpv Cation Channels, Trp (nps) Dipeptides,
Affiliations:
*** IBB - CNR ***
Instituto de Química Médica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
Combinatorial Chemistry Unit, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, Barcelona 08028, Spain
CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona 08028, Spain
Department of Organic Chemistry, University of Barcelona, Barcelona 08028, Spain
IBMC-UMH, Ed. Torregaitán, Av. de la Universidad s/n, 03202 Elche, Spain
Instituto de Qu mica M dica, CSIC, Juan de la Cierva, 3, 28006 Madrid, Spain
References:
Levine, J.D., Alessandri-Haber, N., TRP channels: Targets for the relief of pain (2007) Biochim. Biophys. Acta, 1772, pp. 989-100
Planells-Cases, R., Garcìa-Sanz, N., Morenilla-Palao, C., Ferrer-Montiel, A., Functional aspects and mechanisms of TRPV1 involvement in neurogenic inflammation that leads to thermal hyperalgesia (2005) Pflugers Arch., 451, pp. 151-159
Gunthorpe, M.J., Chizh, B.A., Clinical development of TRPV1 antagonists: Targeting a pivotal point in the pain pathway (2009) Drug Discov. Today, 14, pp. 56-67
Patapoutian, A., Tate, S., Woolf, C.J., Transient receptor potential channels: Targeting pain at the source (2009) Nat. Rev. Drug Discov., 8, pp. 55-68
García-Martínez, C., Morenilla-Palao, C., Planells-Cases, R., Merino, J.M., Ferrer-Montiel, A., Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties (2000) J. Biol. Chem., 275, pp. 32552-32558
García-López, M.T., Herranz, R., González-Muñiz, R., Naranjo, J.R., De Ceballos, M., Del Río, J., Antinociceptive effects in rodents of the dipeptide Lys-Trp(Nps) and related compounds (1986) Peptides, 7, pp. 39-43
Bonache, M.A., García-Martínez, C., García De Diego, L., Carreno, C., Pérez De Vega, M.J., García-López, M.T., Ferrer-Montiel, A., González-Muñiz, R., Old molecule for new receptors: Trp(Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
Szardenings, A.K., Burtoth, T.S., Look, G.C., Campbell, D.A.A., Reductive alkylation procedure applicable to both solution- and solid-phase syntheses of secondary amines (1996) J. Org. Chem., 61, pp. 6720-6722
Shey, J.-Y., Sun, C.-M., Soluble polymer supported synthesis of N,N-di(Boc)-protected guanidines (1998) Synlett, pp. 1423-1425
Del Fresno, M., El-Faham, A., Carpino, L.A., Royo, M., Albericio, F., Substituted guanidines: Introducing diversity in combinatorial chemistry (2000) Org. Lett., 2, pp. 3539-3542
Farrera-Sinfreu, J., Royo, M., Albericio, F., Undesired removal of the Fmoc group by the free ε-amino function of a lysine residue (2002) Tetrahedron Lett., 43, pp. 7813-7815
Levine, J. D., Alessandri-Haber, N., TRP channels: Targets for the relief of pain (2007) Biochim. Biophys. Acta, 1772, pp. 989-100
Gunthorpe, M. J., Chizh, B. A., Clinical development of TRPV1 antagonists: Targeting a pivotal point in the pain pathway (2009) Drug Discov. Today, 14, pp. 56-67
Garc a-Mart nez, C., Morenilla-Palao, C., Planells-Cases, R., Merino, J. M., Ferrer-Montiel, A., Identification of an aspartic residue in the P-loop of the vanilloid receptor that modulates pore properties (2000) J. Biol. Chem., 275, pp. 32552-32558
Garc a-L pez, M. T., Herranz, R., Gonz lez-Mu iz, R., Naranjo, J. R., De Ceballos, M., Del R o, J., Antinociceptive effects in rodents of the dipeptide Lys-Trp (Nps) and related compounds (1986) Peptides, 7, pp. 39-43
Bonache, M. A., Garc a-Mart nez, C., Garc a De Diego, L., Carreno, C., P rez De Vega, M. J., Garc a-L pez, M. T., Ferrer-Montiel, A., Gonz lez-Mu iz, R., Old molecule for new receptors: Trp (Nps) dipeptide derivatives as vanilloid TRPV1 channel blockers (2006) ChemMedChem, 1, pp. 429-438
Szardenings, A. K., Burtoth, T. S., Look, G. C., Campbell, D. A. A., Reductive alkylation procedure applicable to both solution- and solid-phase syntheses of secondary amines (1996) J. Org. Chem., 61, pp. 6720-6722
Shey, J. -Y., Sun, C. -M., Soluble polymer supported synthesis of N, N-di (Boc) -protected guanidines (1998) Synlett, pp. 1423-1425
Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers
Trp(Nps)-Lys-NH(2) derivatives, bearing alkyl or guanidine groups either at the N-terminus or on the Lys side-chain or at both positions were conveniently prepared on solid-phase and evaluated as TRPV1 channel antagonists.
Trp(Nps)-Lys-NH(2) derivatives, bearing alkyl or guanidine groups either at the N-terminus or on the Lys side-chain or at both positions were conveniently prepared on solid-phase and evaluated as TRPV1 channel antagonists.
Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers
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Solid-phase synthesis of new Trp(Nps)-containing dipeptide derivatives as TRPV1 channel blockers
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Bonomo RP, Cucinotta V, Giuffrida A, Impellizzeri G, Magrì A, Pappalardo G, Rizzarelli E, Santoro AM, Tabbì G, Vagliasindi LI
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Impact Factor: 3.003
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Zubrzak P, Banas A, Kaczmarek K, Leplawy MT, Sochacki M, Kowalski ML, Szkudlinska B, Zabrocki J, Di Lello P, Isernia C, Saviano M, Pedone C, Benedetti E
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De Luca S, Morelli G
* Synthesis and characterization of a sulfated and a non-sulfated cyclic CCK8 analogue functionalized with a chelating group for metal labelling (395 views)
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Cucinotta V, Giuffrida A, La Mendola D, Maccarrone G, Puglisi A, Rizzarelli E, Vecchio G
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Mansi R, Tesauro D, De Capua A, Fattorusso R, Carac C, Aloj L, Benedetti E, Morelli G
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Impact Factor: 2.863
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De Luca S, Ragone R, Bracco C, Digilio G, Aloj L, Tesauro D, Saviano M, Pedone C, Morelli G
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De Luca S, Ulhaq S, Dixon M J, EssexJ, Bradley M
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Cucinotta V, Giuffrida A, Grasso G, Maccarrone G, Vecchio G
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Impact Factor: 2.251
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Morelli G, De Luca S, Tesauro D, Saviano M, Pedone C, Dolmella A, Visentin R, Mazzi U
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De Napoli L, De Luca S, Di Fabio G, Messere A, Montesarchio D, Morelli G, Piccialli G, Tesauro D
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De Luca S, Bruno G, Fattorusso R, Isernia C, Pedone C, Morelli G
New synthetic tools for peptide-tetraphenylporphyrin derivatives (326 views)
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Impact Factor: 0.557
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Bonomo RP, Cucinotta V, D'Alessandro F, Impellizzeri G, Maccarrone G, Rizzarelli E, Vecchio G, Carima L, Corradini R, Sartor G, Marchelli R
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Bonomo RP, Di Blasio B, Maccarrone G, Pavone V, Pedone C, Rizzarelli E, Saviano M, Vecchio G
Crystal and Molecular Structure of the [6-Deoxy-6-[(2-(4-imidazolyl)ethyl)amino]cyclomaltoheptaose]copper(II) Ternary Complex with L-Tryptophanate. Role of Weak Forces in the Chiral Recognition Process Assisted by a Metallocyclodextrin (314 views)
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Alberghina M, Brogna A, Mangiameli A, Marletta F, Rizzarelli E, Sammartano S
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* Self‑assembly of thyminyl l‑tryptophanamide (TrpT) building blocks for the potential development of drug delivery nanosystems (13 views)
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Cuocolo A, Pappata S, Zampella E, Assante R
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Calce E, De Luca S
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Calce E, Leone M, Mercurio FA, Monfregola L, De Luca S
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Pica A, Russo Krauss I, Castellano I, La Cara F, Graziano G, Sica F, Merlino A
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Kaprelyants AS, Mukamolova GV, Ruggiero A, Makarov VA, Demina GR, Shleeva MO, Potapov VD, Shramko PA
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Gringeri CV, Menchise V, Rizzitelli S, Cittadino E, Catanzaro V, Dati G, Chaabane L, Digilio G, Aime S
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Galdiero S, Falanga A, Vitiello M, Raiola L, Russo L, Pedone C, Isernia C, Galdiero M
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Galdiero S, Falanga A, Vitiello G, Vitiello M, Pedone C, D'Errico G, Galdiero M
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Staiano M, Saviano M, Herman P, Grycznyski Z, Fini C, Varriale A, Parracino A, Kold AB, Rossi M, D'Auria S
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Impact Factor: 3.003
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Zubrzak P, Banas A, Kaczmarek K, Leplawy MT, Sochacki M, Kowalski ML, Szkudlinska B, Zabrocki J, Di Lello P, Isernia C, Saviano M, Pedone C, Benedetti E
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Impact Factor: 2.425
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De Luca S, Morelli G
* Synthesis and characterization of a sulfated and a non-sulfated cyclic CCK8 analogue functionalized with a chelating group for metal labelling (395 views)
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Impact Factor: 1.652
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Cucinotta V, Giuffrida A, La Mendola D, Maccarrone G, Puglisi A, Rizzarelli E, Vecchio G
* 3-Amino Derivative Of Beta-Cyclodextrin: Thermodynamics Of Copper (ii) Complexes And Exploitation Of Its Enantioselectivity In The Separation Of Amino Acid Racemates By Ligand Exchange Capillary Electrophoresis (350 views)
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Impact Factor: 1.403
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Mansi R, Tesauro D, De Capua A, Fattorusso R, Carac C, Aloj L, Benedetti E, Morelli G
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Impact Factor: 2.863
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Impact Factor: 3.992
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De Luca S, Ulhaq S, Dixon M J, EssexJ, Bradley M
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Impact Factor: 2.326
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Cucinotta V, Giuffrida A, Grasso G, Maccarrone G, Vecchio G
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Impact Factor: 2.251
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Morelli G, De Luca S, Tesauro D, Saviano M, Pedone C, Dolmella A, Visentin R, Mazzi U
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Impact Factor: 1.691
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De Napoli L, De Luca S, Di Fabio G, Messere A, Montesarchio D, Morelli G, Piccialli G, Tesauro D
A facile solid-phase strategy for the synthesis of oligonucleotide- tetraphenylporphyrin conjugates (399 views)
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Impact Factor: 2.15
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De Luca S, Bruno G, Fattorusso R, Isernia C, Pedone C, Morelli G
New synthetic tools for peptide-tetraphenylporphyrin derivatives (326 views)
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Impact Factor: 0.557
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Bonomo RP, Cucinotta V, D'Alessandro F, Impellizzeri G, Maccarrone G, Rizzarelli E, Vecchio G, Carima L, Corradini R, Sartor G, Marchelli R
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Impact Factor: 1.915
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Bonomo RP, Di Blasio B, Maccarrone G, Pavone V, Pedone C, Rizzarelli E, Saviano M, Vecchio G
Crystal and Molecular Structure of the [6-Deoxy-6-[(2-(4-imidazolyl)ethyl)amino]cyclomaltoheptaose]copper(II) Ternary Complex with L-Tryptophanate. Role of Weak Forces in the Chiral Recognition Process Assisted by a Metallocyclodextrin (314 views)
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Impact Factor: 2.736
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Alberghina M, Brogna A, Mangiameli A, Marletta F, Rizzarelli E, Sammartano S
Copper(II) complexes of aminoacids: Gastric acid antisecretory activity in rats (2114 views)
Farmaco Ed Sci, 1982 Dec; 37(12): 805-814.
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Marletta F, Rizzarelli E, Mangiameli A, Brogna A, Sammartano S, Monaco S, Blasi A
Effects of graded doses of copper complexes of L-aminoacids on gastric acid secretion in rats (1341 views)
Boll Soc Ital Biol Sper (ISSN: 0037-8771), 1979 Apr 30; 55(8): 769-775.
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51 Records (49 excluding Abstracts).
Total impact factor: 169.565 (162.301 excluding Abstracts).
Total 5 year impact factor: 163.301 (155.042 excluding Abstracts).
Total impact factor: 169.565 (162.301 excluding Abstracts).
Total 5 year impact factor: 163.301 (155.042 excluding Abstracts).
516 views. Last view on Thursday 23 March 2023, 13:22:55
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