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Santi Mario Spampinato

Full Professor

Department of Pharmacy and Biotechnology

Academic discipline: BIO/14 Pharmacology

Head of Department of Pharmacy and Biotechnology


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Publications prior to 2004

Pubblicazioni scientifiche del periodo: 1993 - 2003

1.     Spampinato S., Paradisi R., Canossa M., Campana G., Frank G., Flamigni C., Ferri S., Immunoreactive Dynorphin A-like material in extracted  human hypothalamic-hypophysial plasma. Life Sciences, 52, 223-230, 1993.

2.     Canossa M., Ventura C., Vaona I., Carboni L., Guarnieri C., Spampinato S., Prodynorphin mRNA expression in adult cultured rat ventricular cardiac myocytes. Biochimica et Biophysica Acta, 1172, 247-250, 1993.

3.     Ventura C., Canossa M., Vaona I., Carboni L., Caldarera Cm., Spampinato S., Guarnieri C. Prodynorphin mRNA is synthesized in adult cultured rat ventricular cardiomyocytes.  Cardioscience 4,  21-24, 1993.

4.     Fontana S., Bernardi P., Pich E.M., Capelli M., Bortoluzzi L., Spampinato S., Canossa M., Relationship between plasma Atrial Natriuretic Factor and opioid peptide levels in healthy subjects and in patients with acute congestive heart failure. European Heart Journal, 14, 219-225, 1993.

5.     Spampinato S., Bachetti T., Carboni L., Ratti E., Van Amsterdam F.T.M., Ferri S., Ca2+ Channel blocking activity of lacidipine and amlodipine in A7r5 vascular smooth muscle cells. European Journal of Pharmacology. Molecular Pharmacology Section, 244, 139-144, 1993.

6.     Ronsisvalle G., Pasquinucci L., Pappalardo M.S., Vittorio F., Fronza G., Romagnoli C., Pistacchio E., Spampinato S., Ferri S., Non-peptide ligands for opioid receptors. Design of K-specific agonists. Journal of Medicinal Chemistry, 36, 1860-1865, 1993.

7.     Berlinck R.G.S., Braekman J.C., Daloze D., Bruno I., Riccio R., Ferri S., Spampinato S., Speroni E., Polycyclic guanidine alkaloids from the marine sponge Crambe Crambe  and Ca++ channel blocker activity of Crambescidin 816. Journal of Natural Products, 56, 1007-1015, 1993.

8.     Melchiorre C., Bolognesi M.L., Chiarini A., Minarini A., Spampinato S., Synthesis and biological activity of some methoctramine-related tetraamines bearing A 11-Acetyl-5,11-Dihydro-6h-Pyrido[2,3-B][1,4]-Benzodiazepin-6-One moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists. Journal of Medicinal Chemistry, 36, 3734-3737, 1993.

9.     Spampinato S., Speroni E., Govoni P., Pistacchio E., Romagnoli C., Murari G., Ferri S., Effect of w-conotoxin and verapamil on antinociceptive, behavioural and thermoregulatory responses to opioids in the rat. European Journal of Pharmacology, 254, 229-238, 1994.

10.  Ventura C., Guarnieri C., Vaona I., Campana G., Pintus G., Spampinato S., Dynorphin gene expression and release in the myocardial cell. Journal of Biological Chemistry, 269, 5384-5386, 1994.

11.  Flamigni F., Campana G., Carboni L., Guarnieri C., Spampinato S., Zinc is required for the expression of ornithine decarboxylase in a difluoromethylornithine-resistant cell line. Biochemistry Journal, 299, 515-519, 1994.

12.  Spampinato S., Canossa M., Carboni L., Campana G., Leanza G., Ferri S., Inhibition of oroopiomelanocortin expression by an Ooigodeoxynucleotide complementary to Beta-endorphin mRNA. Proceedings of the National Academy  Science Usa (PNAS), 91, 8072-8076, 1994.

13.  Flamigni F., Campana G., Carboni L., Rossoni C., Spampinato S., Post-trascriptional inhibition of ornithine decarboxylase induction by zinc in a difluoromethylornithine resistant cell line. Biochimica et Biophysica Acta, 1201, 101-105, 1994.

14.  Minarini A., Bolognesi M.L., Budriesi R., Canossa M., Chiarini A., Spampinato S., Melchiorre C., Design, Synthesys and biological activity of methoctramine. related tetraamines bearing a 11-Acetyl-5,11-Dyhidro-6h-Pyrido[2,3-B] [1,4]-Benzodiazepin-6-One Moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines, Journal of Medicinal Chemistry, 37, 3363-3372, 1994.

15.  Ronsisvalle G., Pappalardo M.S., Prezzavento O., Marrazzo A., Caccamese S., Carboni L., Spampinato S., e-Pmtc, an opioid antagonist bivalent ligand based on N-(Phenylpropyl)-Normetazocine with very high preference for K-sites. Medicinal Chemistry Research, 4, 245-253, 1994.

16.  Fontana F., Bernardi P., Merlo Pich E., Boschi S., De Iasio R., Capelli M., Carboni L., Spampinato S., Endogenous opioid system and Atrial Natriuretic Factor in normotensive offspring of hypertensive parents at rest and during exercise test.  Journal Hypertension, 12, 1285-1290, 1994.

17.  Minarini A., Tumiatti V., Pistacchio E., Spampinato S. , Melchiorre C., Synthesis and biological  activity of 1,4 Dihydropyridine derivatives combining calcium and a1-adrenoceptor antagonistic properties. Medicinal Chemistry Research, 4,153-160, 1994.

18.  Giammona G., Carlisi B., Cavallaro G., Pitarresi G., Spampinato S. A new water-soluble synthetic polymer, a, b-Polyasparthydrazide, as a potential plasma expander and drug carrier. Journal Controlled Release, 29,63-72,1994.

19.  Spampinato S., Canossa S., Campana G., Carboni L., Bachetti T. Estrogen regulation of prodynorphin gene expression in the rat adenohypophisis: effect of the anti-estrogen tamoxifen. Endocrinology ,136, 1589-1594, 1995.


20.  Melchiorre C., Minarini A., Spampinato S., Tumiatti V. Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-Damp. Bioorganic & Medicinal Chemistry Letters 5, 785-790, 1995.


21.  Tumiatti V., Spampinato S., Recanatini M., Minarini A., Melchiorre C., Chiarini A., Budriesi R. Design, synthesis and biological activity of some 4-Damp-related compounds. Bioorganic & Medicinal Chemistry Letters, 5, 2325-2330, 1995.


22.  Puglisi G., Ventura A., Spadaro A., Campana G., Spampinato S. Differential effects of modified Beta-cyclodestrins on pharmacologycal activity and bioavailability of 4-biphenylacetic acid in rats after oral administration. Journal of Pharmacy and Pharmacology, 47,120-123, 1995.

23.  Melchiorre C., Minarini A., Budriesi R., Chiarini A., Spampinato S., Tumiatti V. The design of novel methoctramine-related tetraamines as muscarinic receptor subtype selective antagonists. Life Sciences, 56, 837-844,1995.

24.  Ronsisvalle G., Prezzavento O., Pasquinucci L., Marrazzo A., Vittorio F., Gomez-Vidal J.A., Carboni L., Spampinato S. CCB, a novel specific K opioid agonist, which discriminates between opioid and s1  recognition sites. Life Sciences, 56, 837-844, 1995.

25.  Dei S., Bellucci C., Ghelardini C., Romanelli M.N., Spampinato S. Synthesis, Characterization and pharmacological profile of tropicamide enantiomers. Life Sciences 58, 2147-2153, 1996.

26.  Giammona G., Pitarresi G., Tomarchio V., Spampinato S., Govoni P., Campana, G. New hydrogel matrices based on chemical crosslinked a, b- polyaspartazide : synthesis, characterization and in vivo biocompatibility studies. International Journal of Pharmaceutics 127, 165-175, 1996.

27.  Santagati M., Modica M., Santagati A., Russo F., Spampinato S. Synthesis of Aminothienopyrimidine And Thienotriazolopyrimidine derivatives as potential anticonvulsant agents. Pharmazie, 51, 7-11, 1996.

28.  Carboni L., Campana G., Cacciaguerra S., Speroni E., Murari G., Ronsisvalle G., Spampinato S. Agonist binding properties for recombinant Kappa opioid receptors expressed in CHO-K1 cells. Ann. N.Y. Acad. Sci. 812, 203-205, 1997.

29.  Fontana F., Bernardi P., Spampinato S., Boschi S., De Iasio R., Grossi G. Pressor effects of endogenous opioid system during acute episodes of blood pressure increases in hypertensive patients. Hypertension. 29, 105-110, 1997.

30.  Giardinà D., Crucianelli M., Gulini U., Marucci G., Melchiorre C., Spampinato S. Synthesis and a1-antagonist activity of new prazosin- and benextramine-related tetraamine disulfides. European Journal of Medicinal Chemistry 32, 9-20, 1997.

31.  Fontana F., Bernardi P., Merlo Pich E., Boschi S., De Iasio R., Spampinato S., Grossi G. Opioid peptide modulation of circulatory and endocrine response to mental stress in humans. Peptides 18, 169-175, 1997.

32.  Ucar H., Cacciaguerra S., Spampinato S., Van Derpoorten K., Isa M., Kanyonyo M., Poupert J. 2(3H)-Benzoxazolone and 2(3H)-Benzothiazolone derivatives : novel, potent and selective s1 receptor ligands. European Journal of Pharmacology, 355, 267-273, 1997.

33.  Fontana F., Bernardi P., Merlo Pich E., Boschi S., De Iasio R., Spampinato S.  Endogenous opioid peptides and mental stress in congestive heart failure patients. Peptides, 19, 21-26, 1998.

34.  Ucar H., Van Derpoorten K., Cacciaguerra S., Spampinato S., Stables J., Depovere P., Isa M., Masereel B., Delarge J., Poupert J.H. Synthesis and anticonvulsant activity of 2(3H)-Benzoxazolone and 2(3H)-Benzothiazolone derivatives. Journal of Medicinal Chemistry, 41, 1138-1145, 1998.

35.  Fresta M., Chillemi R., Spampinato S., Sciuto S., Puglisi G. Liposomal Delivery Of A 30-Mer antisense oligodeoxynucleotide to inhibit proopiomelanocortin expression. Journal of Pharmaceutical Sciences 87, 616-625, 1998.

36.  Quaglia W., Giannella M., Piergentili A., Pigini N., Brasili L., Di Toro R., Rossetti L., Spampinato S., Melchiorre C. 1'-Benzyl-3,4-Dihydrospiro[2h-1-Benzothiopyran-2,4'-Piperidine] (Spipethiane), a potent and highly selective s1 ligand. Journal of Medicinal Chemistry, 41, 1557-1560, 1998.

37.  Ronsisvalle G., Marrazzo A., Prezzavento O., Pasquinucci L., Vittorio F., Pittala' V., Pappalardo M.S., Cacciaguerra S., Spampinato S. (+)-Cis-N-Ethyleneamino-N-Normetazocine derivatives. Novel and selective s ligands with antagonist properties. Journal of Medicinal Chemistry, 41, 1574-1580. 1998.

38.  Bolognesi M.L., Minarini A., Budriesi R., Cacciaguerra S., Chiarini A., Spampinato S., Tumiatti V., Melchiorre C. Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists. Journal of Medicinal Chemistry, 41, 4150-4160. 1998.

39.  Di Toro R. Campana G., Sciarretta V., Murari G. Spampinato S. Regulation of delta opioid receptors by delta-9-tetrahydrocannabinol in NG 108-15 hybrid cells. Life Sciences 63, Pl 197-204, 1998.

40.  Fontana F., Bernardi P., Merlo Pich E., Tartuferi L., Boschi S., De Iasio R., Spampinato S. Opioid peptides in response to mental stress in asymptomatic dilated cardiomyopathy. Peptides, 19, 1147-1153, 1998.

41.  Budriesi R., Aicardi G., Campana G., Spampinato S., Zaza A., Bisi A., Rampa A., Valenti P., Chiarini A. Selective cardiodepressant activity of fluodipine, a fluorenone-1,4-dihydropyridine derivative. European Journal of Pharmacology, 359, 161-170, 1998.

42.  Bucolo C., Campana G., Di Toro R., Cacciaguerra S., Spampinato S. s1 recognition sites in rabbit iris-ciliary body: topical s1-site agonists lower intraocular pressure. Journal of Pharmacology and Experimental Therapeutics, 289, 271-278, 1999.

43.  Spampinato S., Falcucci B., Cacciaguerra S., Campana G., Murari G. Characterization of a putative calcitonin receptor in IMR 32 human neuroblastoma cells. Neuroscience Letters, 273, 167-170, 1999.

44.  Ronsisvalle G., Pasquinucci L., Pittala' V., Marrazzo A., Prezzavento O., Di Toro R., Falcucci B., Spampinato S. Nonpeptide analogues of dynorphin A(1-8): design, synthesis and pharmacological evaluation of Kappa-selective agonists. Journal of Medicinal Chemistry 43, 2992-3004, 2000.

45.  Ronsisvalle G., Marrazzo A., Prezzavento O., Pasquinucci L., Falcucci B., Di Toro R., Spampinato S. Substituted 1-Phenyl-2-Cyclopropylmethylamines with high affinity and selectivity for sigma sites. Bioorganic & Medicinal Chemistry 8, 1503-1513, 2000.

46.  Pasquariello A., Di Toro R., Nyberg F., Spampinato S. Down-regulation of delta opioid receptor mRNA by an anabolic steroid in neuronal hybrid cells. Neuroreport, 11, 863-867, 2000.

47.  Di Toro R., Campana G., Murari G., Spampinato S. Effects of specific bile acids on c-fos messenger RNA levels in human colon carcinoma Caco-2 cells. European Journal of Pharmaceutical Sciences, 11, 291-298, 2000.

48.  Cardillo G, Gentilucci L, Melchiorre P, Spampinato S. Synthesis and binding activity of Endomorphin-1 analogues containing beta-amino acids. Biorgonic & Medicinal Chemistry Lettetter 10, 2755-2758, 2000.

49.  Fontana F., Bernardi P., Pich E.M., Tartuferi L., Boschi S., Spampinato S. Opioid peptide modulation of circulatory response to hyperventilation in humans. Peptides 21: 1223-1230, 2000.

50.  Ronsisvalle G, Prezzavento O, Marrazzo A, Vittorio F, Bousquet E, Di Toro R, Spampinato S. Synthesis and binding affinity of cis-(-)- and cis-(+)-N-Ethyleneamino-N-Nordeoxymetazocine and Cis-(-)-N-Normetazocine Analogues at sigma(1), sigma(2) and Kappa opioid receptors. European Journal of Pharmaceutical  Sciences 12, 277-284, 2001.

51.  Budriesi R., Cacciaguerra S., Di Toro R., Bolognesi M.L., Chiarini A., Minarini A., Rosini M., Spampinato S., Tumiatti V., Melchiorre C. Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines. British Journal of Pharmacolology 132, 1009-1016, 2001.

52.  Fontana F., Bernardi P., Tartuferi L., Boschi S., Di Toro R., Spampinato S. Opioid peptides attenuate blood pressure increase in acute respiratory failure. Peptides 22: 631-637, 2001.

53.  Spampinato S., Di Toro R., Qasem A.R. Nociceptin-induced internalization of the ORL-1 receptor in human neuroblastoma cells. Neuroreport 12, 3159-3163, 2001.

  1. Angeli P, Marucci G, Buccioni M, Piergentili A, Giannella M, Quaglia W, Pigni M, Cantalamessa F, Nasuti C, Novi F, Maggio R, Qasem Ar, Spampinato S. Deoxamuscaroneoxime derivatives as useful muscarinic agonists to explore the muscarinic subsite: demox, a modulator of orthosteric and allosteric sites at cardiac muscarinic M-2 receptors. Life Sciences 70, 1427-1446, 2002.


  1. Loizzo A, Loizzo S, Lopez L, D'amore A, Renzi P, Spampinato S, Di Carlo S, Bacosi A, Zuccaro P, Pacifici R. Naloxone prevents cell-mediated immune alterations in adult mice following repeated mildstress in the neonatal period. British Journal of Pharmacology 135, 1219-1226, 2002.


  1. Mouithys-Mickalad A, Poupaert Jh, Spampinato S, Lesieur D. Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3h)-benzothiazolones as mixed sigma/5-HT1a ligands. Bioorganic & Medicinal Chemistry Letters 12, 1149-1152, 2002.


  1. Fontana F, Bernardi P, Spampinato S, Di Toro R, Bugiardini R. Beta-Endorphin modulation of pressor response to hyperventilation in hypertensive patients. Peptides 23, 911-918, 2002.


  1. Santagati Na, Prezzavento O, Bousquet E, Ronsisvalle G, Spampinato S. Synthesis and spasmolytic action of 2-substituted thienopyrimidin-4-one derivatives. Journal of Pharmacy and Pharmacology  54, 717-728, 2002.


  1. Cardillo G, Gentilucci L, Qasem Ar, Sgarzi F, Spampinato S. Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. Journal of Medicinal Chemistry 45, 2571-2578, 2002.


  1. Ronsisvalle G, Prezzavento O, Marrazzo A, Vittorio F, Massimino M, Murari G, Spampinato S. Synthesis of (+)-cis-n-(4-isothiocyanatobenzyl)-n-normetazocine, an isothiocyanate derivative of n-benzylnormetazocine as acylant agent for the sigma(1) receptor. Journal of Medicinal Chemistry 45, 2662-2665, 2002.


  1. Spampinato S, Di Toro R, Alessandri M, Murari G. Agonist-induced internalization and desensitization of the human nociceptin receptor expressed in CHO cells. Cellular and Molecular Life Sciences 59, 2172-2183, 2002.


  1. Campana G, Bucolo C, Murari G, Spampinato S. Ocular hypotensive action of topical flunarizine in the rabbit: role of sigma(1) recognition sites. Journal of Pharmacology and Experimental Therapeutics 303, 1086-1094, 2002.


  1. Cardillo G, Gentilucci L, Tolomelli A, Qasem AR, Spampinato S, Calienni M. Conformational analysis and mu-opioid receptor affinity of short peptides, endomorphin models in a low polarity solvent. Org Biomol Chem. 2003 Sep 7;1(17):3010-4.


  1. Cardillo G, Gentilucci L, Tolomelli A, Calienni M, Qasem AR, Spampinato S. Stability against enzymatic hydrolysis of endomorphin-1 analogues containing beta-proline. Org Biomol Chem. 2003 May 7;1(9):1498-502.


  1. Spampinato S, Qasem AR, Calienni M, Murari G, Gentilucci L, Tolomelli A, Cardillo G. Antinociception by a peripherally administered novel endomorphin-1 analogue containing beta-proline. Eur J Pharmacol. 2003 May 23;469(1-3):89-95.