L-368,899
L-368,899 is a drug used in scientific research which acts as a selective antagonist of the oxytocin receptor, with good selectivity over the related vasopressin receptors.[1] Unlike related drugs such as the peripherally selective L-371,257, the oral bioavailabity is high and the brain penetration of L-368,899 is rapid, with selective accumulation in areas of the limbic system. This makes it a useful tool for investigating the centrally mediated roles of oxytocin, such as in social behaviour and pair bonding, and studies in primates have shown L-368,899 to reduce a number of behaviours such as food sharing, sexual activity and caring for infants, demonstrating the importance of oxytocinergic signalling in mediating these important social behaviours.[2][3]
See also
References
- ↑ Williams PD, Anderson PS, Ball RG, Bock MG, Carroll L, Chiu SH, Clineschmidt BV, Culberson JC, Erb JM, Evans BE (March 1994). "1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor". Journal of Medicinal Chemistry 37 (5): 565–71. doi:10.1021/jm00031a004. PMID 8126695.
- ↑ Boccia ML, Goursaud AP, Bachevalier J, Anderson KD, Pedersen CA (September 2007). "Peripherally administered non-peptide oxytocin antagonist, L368,899, accumulates in limbic brain areas: a new pharmacological tool for the study of social motivation in non-human primates". Hormones and Behavior 52 (3): 344–51. doi:10.1016/j.yhbeh.2007.05.009. PMC 2712625. PMID 17583705.
- ↑ Smith AS, Agmo A, Birnie AK, French JA (February 2010). "Manipulation of the oxytocin system alters social behavior and attraction in pair-bonding primates, Callithrix penicillata". Hormones and Behavior 57 (2): 255–62. doi:10.1016/j.yhbeh.2009.12.004. PMC 2824532. PMID 20025881.
|
---|
| CGRP | |
---|
| Cholecystokinin | |
---|
| CRH | |
---|
| Galanin | |
---|
| MCH | | |
---|
| |
- Agonists: Melanin concentrating hormone
|
---|
|
---|
| Melanocortin | | |
---|
| | |
---|
| | |
---|
| | |
---|
| | |
---|
| Unsorted |
- Agonists: Alsactide
- Codactide
- Giractide
- Norleusactide
- Seractide
- Tosactide
- Tricosactide
- Tridecactide
|
---|
|
---|
| Neuropeptide S | |
---|
| Neuropeptide Y | |
---|
| Neurotensin | |
---|
| Opioid | See here instead. |
---|
| Orexin | |
---|
| Oxytocin | |
---|
| Tachykinin | |
- Agonists: Substance P
Antagonists: Aprepitant
- Befetupitant
- Burapitant
- Casopitant
- CI-1021
- CP-96,345
- CP-99,994
- CP-122,721
- Dapitant
- Ezlopitant
- Figopitant
- FK-888
- Fosaprepitant
- GR-203,040
- GW-597,599
- HSP-117
- L-733,060
- L-741,671
- L-743,310
- L-758,298
- Lanepitant
- LY-306,740
- Maropitant
- Netupitant
- NKP-608
- Nolpitantium besilate
- Orvepitant
- Rolapitant
- RP-67,580
- SDZ NKT 343
- Serlopitant
- Telmapitant
- Vestipitant
- Vofopitant
|
---|
| | |
---|
| | |
---|
|
---|
| Vasopressin | |
---|
| See also: Peptidergics |
|