Ligand Id: 206
Ligand name mesulergine

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 0
Rotatable bonds 3
Topological polar surface area 53.93
Molecular weight 361.18
XLogP 2.1
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

Summary Biological activity References Structure Similar ligands Radio analogues
References
1. Hameg, A., Bayle, F., Nuss, P., Dupuis, P., Garay, R. P. and Dib, M. (2003)
Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes.
Biochem Pharmacol, 65: 435-440. [PMID:12527336]
2. Knight, A. R., Misra, A., Quirk, K., Benwell, K., Revell, D., Kennett, G. and Bickerdike, M. (2004)
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
Naunyn Schmiedebergs Arch Pharmacol, 370: 114-123. [PMID:15322733]
3. Sleight, A. J., Stam, N. J., Mutel, V. and Vanderheyden, P. M. (1996)
Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities.
Biochem Pharmacol, 51: 71-76. [PMID:8534270]
4. Johnson, M. P., Loncharich, R. J., Baez, M. and Nelson, D. L. (1994)
Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines.
Mol Pharmacol, 45: 277-286. [PMID:8114677]
5. Kovacs, A., Gacsalyi, I., Wellmann, J., Schmidt, E., Szucs, Z., Dubreuil, V., Nicolas, J. P., Boutin, J., Bozsing, D., Egyed, A., Tihanyi, K., Spedding, M. and Szenasi, G. (2003)
Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist.
Cardiovasc Drugs Ther, 17: 427-434. [PMID:15107597]
6. Wainscott, D. B., Cohen, M. L., Schenck, K. W., Audia, J. E., Nissen, J. S., Baez, M., Kursar, J. D., Lucaites, V. L. and Nelson, D. L. (1993)
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
Mol Pharmacol, 43: 419-426. [PMID:8450835]
7. Wainscott, D. B., Sasso, D. A., Kursar, J. D., Baez, M., Lucaites, V. L. and Nelson, D. L. (1998)
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
Naunyn Schmiedebergs Arch Pharmacol, 357: 17-24. [PMID:9459568]
8. Herrick-Davis, K., Egan, C. and Teitler, M. (1997)
Activating mutations of the serotonin 5-HT2C receptor.
J Neurochem, 69: 1138-1144. [PMID:9282936]
9. Monsma, F. J., Shen, Y., Ward, R. P., Hamblin, M. W. and Sibley, D. R. (1993)
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Mol Pharmacol, 43: 320-327. [PMID:7680751]
10. Kohen, R., Metcalf, M. A., Khan, N., Druck, T., Huebner, K., Lachowicz, J. E., Meltzer, H. Y., Sibley, D. R., Roth, B. L. and Hamblin, M. W. (1996)
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
J Neurochem, 66: 47-56. [PMID:8522988]
11. Boess, F. G., Monsma, F. J., Carolo, C., Meyer, V., Rudler, A., Zwingelstein, C. and Sleight, A. J. (1997)
Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Neuropharmacology, 36: 713-720. [PMID:9225298]
12. Boess, F. G., Riemer, C., Bos, M., Bentley, J., Bourson, A. and Sleight, A. J. (1998)
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
Mol Pharmacol, 54: 577-583. [PMID:9730917]
13. Boess, F. G., Monsma, F. J., Meyer, V., Zwingelstein, C. and Sleight, A. J. (1997)
Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
Mol Pharmacol, 52: 515-523. [PMID:9284367]
14. Shen, Y., Monsma, F. J., Metcalf, M. A., Jose, P. A., Hamblin, M. W. and Sibley, D. R. (1993)
Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
J Biol Chem, 268: 18200-18204. [PMID:8394362]
15. Plassat, J. L., Amlaiky, N. and Hen, R. (1993)
Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Mol Pharmacol, 44: 229-236. [PMID:8394987]
16. Krobert, K. A., Bach, T., Syversveen, T., Kvingedal, A. M. and Levy, F. O. (2001)
The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Naunyn Schmiedebergs Arch Pharmacol, 363: 620-632. [PMID:11414657]
17. Jasper, J. R., Kosaka, A., To, Z. P., Chang, D. J. and Eglen, R. M. (1997)
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Br J Pharmacol, 122: 126-132. [PMID:9298538]
18. Bard, J. A., Zgombick, J., Adham, N., Vaysse, P., Branchek, T. A. and Weinshank, R. L. (1993)
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
J Biol Chem, 268: 23422-23426. [PMID:8226867]
19. Thomas, D. R., Gittins, S. A., Collin, L. L., Middlemiss, D. N., Riley, G., Hagan, J., Gloger, I., Ellis, C. E., Forbes, I. T. and Brown, A. M. (1998)
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Br J Pharmacol, 124: 1300-1306. [PMID:9720804]