Synonym
p-MPPI HCl; p-MPPI hydrochloride;
IUPAC/Chemical Name
4-Iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)benzamide monohydrochloride
InChi Key
PBPBIDMIRMWUCI-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H27IN4O2.ClH/c1-32-23-7-3-2-6-22(23)29-17-14-28(15-18-29)16-19-30(24-8-4-5-13-27-24)25(31)20-9-11-21(26)12-10-20;/h2-13H,14-19H2,1H3;1H
SMILES Code
O=C(N(CCN1CCN(C2=CC=CC=C2OC)CC1)C3=NC=CC=C3)C4=CC=C(I)C=C4.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors.
In vivo activity:
The present study examined p-MPPI's potential as an antagonist of the sleep and waking responses elicited by 8-OH-DPAT. Also, the experiments explored the ability of p-MPPI to block behavioural reactions of the 5-HT syndrome induced by 8-OH-DPAT, and whether p-MPPI induced any behavioural effects of its own. This study demonstrated that pre-treatment with p-MPPI (5 mg/kg intraperitoneal (i.p.)) 30 min before 8-OH-DPAT (0.375 mg/kg subcutaneously (s.c.)) reduced the effect of 8-OH-DPAT on waking and REM sleep. Also, p-MPPI (5 and 10 mg/kg i.p.) reduced the effect of 8-OH-DPAT on locomotion and partially or completely antagonized hindlimb abduction and flat body posture. No overt behavioural change was produced by p-MPPI alone.
Reference: Behav Brain Res. 2001 Jun;121(1-2):181-7. https://pubmed.ncbi.nlm.nih.gov/11275295/
|
Solvent |
mg/mL |
mM |
| Solubility |
| Water |
3.3 |
5.75 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
578.88
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Sørensen E, Grønli J, Bjorvatn B, Ursin R. The selective 5-HT(1A) receptor antagonist p-MPPI antagonizes sleep--waking and behavioural effects of 8-OH-DPAT in rats. Behav Brain Res. 2001 Jun;121(1-2):181-7. doi: 10.1016/s0166-4328(01)00163-2. PMID: 11275295.
2. Cao BJ, Rodgers RJ. Anxiolytic-like profile of p-MPPI, a novel 5HT1A receptor antagonist, in the murine elevated plus-maze. Psychopharmacology (Berl). 1997 Feb;129(4):365-71. doi: 10.1007/s002130050202. PMID: 9085406.
In vivo protocol:
1. Sørensen E, Grønli J, Bjorvatn B, Ursin R. The selective 5-HT(1A) receptor antagonist p-MPPI antagonizes sleep--waking and behavioural effects of 8-OH-DPAT in rats. Behav Brain Res. 2001 Jun;121(1-2):181-7. doi: 10.1016/s0166-4328(01)00163-2. PMID: 11275295.
2. Cao BJ, Rodgers RJ. Anxiolytic-like profile of p-MPPI, a novel 5HT1A receptor antagonist, in the murine elevated plus-maze. Psychopharmacology (Berl). 1997 Feb;129(4):365-71. doi: 10.1007/s002130050202. PMID: 9085406.
1: Naumenko VS, Kondaurova EM, Popova NK. Central 5-HT3 receptor-induced hypothermia in mice: interstrain differences and comparison with hypothermia mediated via 5-HT1A receptor. Neurosci Lett. 2009 Nov 6;465(1):50-4. doi: 10.1016/j.neulet.2009.09.005. Epub 2009 Sep 6. PubMed PMID: 19735696.
2: Fiske E, Portas CM, Grønli J, Sørensen E, Bjorvatn B, Bjørkum AA, Ursin R. Increased extracellular 5-HT but no change in sleep after perfusion of a 5-HT1A antagonist into the dorsal raphe nucleus of rats. Acta Physiol (Oxf). 2008 May;193(1):89-97. Epub 2007 Dec 14. PubMed PMID: 18081887.
3: Hassanain M, Bhatt S, Siegel A. Differential modulation of feline defensive rage behavior in the medial hypothalamus by 5-HT1A and 5-HT2 receptors. Brain Res. 2003 Aug 15;981(1-2):201-9. PubMed PMID: 12885442.
4: Winsauer PJ, Moerschbaecher JM. Differential effects of 5-HT agonists and antagonists on the repeated acquisition and performance of response sequences in monkeys. Behav Pharmacol. 2000 Nov;11(7-8):535-53. PubMed PMID: 11198126.
5: Errico M, Crozier RA, Plummer MR, Cowen DS. 5-HT(7) receptors activate the mitogen activated protein kinase extracellular signal related kinase in cultured rat hippocampal neurons. Neuroscience. 2001;102(2):361-7. PubMed PMID: 11166122.
6: Bjorvatn B, Fornal CA, Martín FJ, Metzler CW, Jacobs BL. Venlafaxine and its interaction with WAY 100635: effects on serotonergic unit activity and behavior in cats. Eur J Pharmacol. 2000 Sep 15;404(1-2):121-32. PubMed PMID: 10980270.
7: Roumy M, Zajac J. Neuropeptide FF selectively attenuates the effects of nociceptin on acutely dissociated neurons of the rat dorsal raphe nucleus. Brain Res. 1999 Oct 23;845(2):208-14. PubMed PMID: 10536200.
8: Ahlemeyer B, Glaser A, Schaper C, Semkova I, Krieglstein J. The 5-HT1A receptor agonist Bay x 3702 inhibits apoptosis induced by serum deprivation in cultured neurons. Eur J Pharmacol. 1999 Apr 9;370(2):211-6. PubMed PMID: 10323272.
9: Matuszewich L, Lorrain DS, Trujillo R, Dominguez J, Putnam SK, Hull EM. Partial antagonism of 8-OH-DPAT'S effects on male rat sexual behavior with a D2, but not a 5-HT1A, antagonist. Brain Res. 1999 Feb 27;820(1-2):55-62. PubMed PMID: 10023030.
10: Lorrain DS, Matuszewich L, Hull EM. 8-OH-DPAT influences extracellular levels of serotonin and dopamine in the medial preoptic area of male rats. Brain Res. 1998 Apr 20;790(1-2):217-23. PubMed PMID: 9593901.
11: Wolff MC, Leander JD. Differentiation of 5-HT1A receptor ligands by drug discrimination. Eur J Pharmacol. 1997 Aug 27;333(2-3):113-22. PubMed PMID: 9314023.
12: Shaikh MB, De Lanerolle NC, Siegel A. Serotonin 5-HT1A and 5-HT2/1C receptors in the midbrain periaqueductal gray differentially modulate defensive rage behavior elicited from the medial hypothalamus of the cat. Brain Res. 1997 Aug 15;765(2):198-207. PubMed PMID: 9313892.
