5-CT

Ligand id: 4

Name: 5-CT

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 3
Topological polar surface area 84.9
Molecular weight 203.11
XLogP 0.02
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

References
1. Adham N, Bard JA, Zgombick JM, Durkin MM, Kucharewicz S, Weinshank RL, Branchek TA. (1997)
Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog.
Neuropharmacology36: 569-576. [PMID:9225282]
2. Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA. (1993)
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
Proc Natl Acad Sci U S A90: 408-412. [PMID:8380639]
3. Bai F, Yin T, Johnstone EM, Su C, Varga G, Little SP, Nelson DL. (2004)
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
Eur J Pharmacol484: 127-139. [PMID:14744596]
4. Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL. (1993)
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
J Biol Chem268: 23422-23426. [PMID:8226867]
5. Boess FG, Monsma FJ, Carolo C, Meyer V, Rudler A, Zwingelstein C, Sleight AJ. (1997)
Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells.
Neuropharmacology36: 713-720. [PMID:9225298]
6. Boess FG, Monsma FJ, Sleight AJ. (1998)
Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
J Neurochem71: 2169-2177. [PMID:9798944]
7. Egan C, Grinde E, Dupre A, Roth BL, Hake M, Teitler M, Herrick-Davis K. (2000)
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
Synapse35: 144-150. [PMID:10611640]
8. Erlander MG, Lovenberg TW, Baron BM, de Lecea L, Danielson PE, Racke M, Slone AL, Siegel BW, Foye PE, Cannon K et al.. (1993)
Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.
Proc. Natl. Acad. Sci. U.S.A.90 (8): 3452-6. [PMID:7682702]
9. Grailhe R, Grabtree GW, Hen R. (2001)
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
Eur J Pharmacol418: 157-167. [PMID:11343685]
10. Hamblin MW, Metcalf MA. (1991)
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Mol Pharmacol40: 143-148. [PMID:1652050]
11. Jasper JR, Kosaka A, To ZP, Chang DJ, Eglen RM. (1997)
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Br J Pharmacol122: 126-132. [PMID:9298538]
12. Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, 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 Pharmacol370: 114-123. [PMID:15322733]
13. Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW. (1996)
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
J Neurochem66: 47-56. [PMID:8522988]
14. Krobert KA, Bach T, Syversveen T, Kvingedal AM, Levy FO. (2001)
The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution.
Naunyn Schmiedebergs Arch Pharmacol363: 620-632. [PMID:11414657]
15. Kursar JD, Nelson DL, Wainscott DB, Baez M. (1994)
Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor.
Mol Pharmacol46: 227-234. [PMID:8078486]
16. Leysen JE, Gommeren W, Heylen L, Luyten WH, Van de Weyer I, Vanhoenacker P, Haegeman G, Schotte A, Van Gompel P, Wouters R, Lesage AS. (1996)
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Mol Pharmacol50: 1567-1580. [PMID:8967979]
17. Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG. (1993)
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.
Proc Natl Acad Sci U S A90: 2184-2188. [PMID:8384716]
18. Maroteaux L, Saudou F, Amlaiky N, Boschert U, Plassat JL, Hen R. (1992)
Mouse 5HT1B serotonin receptor: cloning, functional expression, and localization in motor control centers.
Proc Natl Acad Sci U S A89: 3020-3024. [PMID:1557407]
19. Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R. (1993)
Mouse 5-hydroxytryptamine 5A and 5-hydroxytryptamine 5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
Mol. Pharmacol.43: 313-319. [PMID:8450829]
20. McAllister G, Charlesworth A, Snodin C, Beer MS, Noble AJ, Middlemiss DN, Iversen LL, Whiting P. (1992)
Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.
Proc Natl Acad Sci U S A89: 5517-5521. [PMID:1608964]
21. Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR. (1993)
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
Mol Pharmacol43: 320-327. [PMID:7680751]
22. Newman-Tancredi A, Conte C, Chaput C, Verriele L, Audinot-Bouchez V, Lochon S, Lavielle G, Millan MJ. (1997)
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
Naunyn Schmiedebergs Arch Pharmacol355: 682-688. [PMID:9205951]
23. Newman-Tancredi A, Gavaudan S, Conte C, Chaput C, Touzard M, Verriele L, Audinot V, Millan MJ. (1998)
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
Eur J Pharmacol355: 245-256. [PMID:9760039]
24. Newman-Tancredi A, Verriele L, Chaput C, Millan MJ. (1998)
Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists.
Naunyn Schmiedebergs Arch Pharmacol357: 205-217. [PMID:9550290]
25. Newman-Tancredi A, Wootton R, Strange PG. (1992)
High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells.
Biochem J285: 933-938. [PMID:1386736]
26. Parker EM, Izzarelli DG, Lewis-Higgins L, Palmer D, Shapiro RA. (1996)
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
J Neurochem67: 2096-2103. [PMID:8863519]
27. Plassat JL, Amlaiky N, Hen R. (1993)
Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase.
Mol Pharmacol44: 229-236. [PMID:8394987]
28. Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M. (1994)
Cloning and characterisation of the human 5-HT5A serotonin receptor.
FEBS Lett.355: 242-246. [PMID:7988681]
29. Ruat M, Traiffort E, Leurs R, Tardivel-Lacombe J, Diaz J, Arrang JM, Schwartz JC. (1993)
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
Proc Natl Acad Sci U S A90: 8547-8551. [PMID:8397408]
30. Shen Y, Monsma FJ, Metcalf MA, Jose PA, Hamblin MW, Sibley DR. (1993)
Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
J Biol Chem268: 18200-18204. [PMID:8394362]
31. Thomas DR, Gittins SA, Collin LL, Middlemiss DN, Riley G, Hagan J, Gloger I, Ellis CE, Forbes IT, Brown AM. (1998)
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.
Br J Pharmacol124: 1300-1306. [PMID:9720804]
32. Wainscott DB, Cohen ML, Schenck KW, Audia JE, Nissen JS, Baez M, Kursar JD, Lucaites VL, Nelson DL. (1993)
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
Mol Pharmacol43: 419-426. [PMID:8450835]
33. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR. (1992)
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1Dα and 5-HT1Dβ.
Proc. Natl. Acad. Sci. U.S.A.89: 3630-3634. [PMID:1565658]
34. Weiss HM, Haase W, Michel H, Reilander H. (1995)
Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization.
FEBS Lett377: 451-456. [PMID:8549774]