[D- MET2 , PRO5 ]-ENKEPHALINAMIDE

Names

[ Name ]:
[D- MET2 , PRO5 ]-ENKEPHALINAMIDE

[Synonym ]:
H-Tyr-D-Met-Gly-Phe-Pro-NH2
L-tyrosyl-D-methionyl-glycyl-L-phenylalanyl-L-proline amide
Tyr-D-Met-Gly-Phe-Pro-NH2

Biological Activity

[Description]:

(D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Research Areas >> Others

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

[In Vivo]

(D-Met2,Pro5)-Enkephalinamide (intravenous injection; 0.25 and 0.5 mg/kg; once) leads to the decreasement of prolactin (PRL) secretion in lactating rats[2]. Animal Model: Wistar lactating rats[2] Dosage: 0.25 and 0.5 mg/kg Administration: Intravenous injection; 0.25 and 0.5 mg/kg; once Result: Decreased plasma PRL levels 15 min after the administration in continuously lactating rats. Produced a marked depression in plasma PRL concentration in non-deprived lactating mothers.

Chemical & Physical Properties

[ Density]:
1.31g/cm3

[ Boiling Point ]:
1065ºC at 760 mmHg

[ Molecular Formula ]:
C₃₀H₄₀N₆O₆S

[ Molecular Weight ]:
612.74000

[ Flash Point ]:
597.9ºC

[ Exact Mass ]:
612.27300

[ PSA ]:
233.71000

[ LogP ]:
4.12870

[ Index of Refraction ]:
1.616

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TW3583000

CHEMICAL NAME :: L-Prolinamide, L-tyrosyl-D-methionylglycyl-L-phenylalanyl-

CAS REGISTRY NUMBER :: 63307-63-1

LAST UPDATED :: 199706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C30-H40-N6-O6-S

MOLECULAR WEIGHT :: 612.82

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 510 mg/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 118 mg/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1700 mg/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 278 mg/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning

REFERENCE :: PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987

Synthetic Route

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Related Compounds

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