PT-141 is a synthetic variant of the naturally occurring peptide hormone alpha-melanocyte stimulating hormone (α-MSH)¹ and has been proven as an effective agent for the improvement of sexual dysfunction in both male and female animal test subjects².

Naturally occurring α-MSH acts as an agonist of melanocortin receptors MC1, MC3, and MC4; receptor MC1 has been shown to be responsible for skin pigmentation effects, while MC3 and MC4 are responsible for effects on appetite, metabolism, and sexual activity³. Using this understanding of the native peptide, PT-141 was developed as an agent meant only to bind melanocortin receptors MC3 and MC4, thereby acting as a selective stimulator of cellular metabolic and erectile effects⁴.

PT-141 has been shown to be a lipolytic (fat cell-destroying) agent⁵, a suppressant of appetite⁶, and a stimulant of libido in animal test subjects⁴. PT-141 has demonstrated great efficacy in reducing caloric intake, while eliminating cholesterol and fat stores in obese mice through its targeted metabolic action⁷.

Product Comparison

PT-141 is structurally similar to the biosynthetic peptide hormone Melanotan II, but has shown to be a potent binding agent of MC3 and MC4 only, demonstrating no affinity for MC1. In animal tests, PT-141 has proven quite effective at correcting sexual dysfunction², while Melanotan II induces an additional effect on skin tone.

Unlike other agents that have an effect on erectile response (e.g. Viagra), PT-141 performs no action on the vascular system, but rather induces arousal and heightens sexual desire via the nervous system – binding important receptors in the brain⁸.

Melatonan I is also structurally similar to PT-141, both being synthetic analogues of α-MSH, but Melanotan I is only active in binding the MC1 receptor³, thereby producing skin tanning effects and neglecting any stimulation of sexual response. Though these agents look alike, they could not be more separate in function.

Synonyms:

PT 141; PT141; Bremelanotide; Bremelin

Peer-Reviewed Sources:

Molinoff, P. B., Shadiack, A. M., Earle, D., Diamond, L. E., & Quon, C. Y. (2003). PT‐141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994(1), 96-102. ↩︎
Diamond, L. E., Earle, D. C., Heiman, J. R., Rosen, R. C., Perelman, M. A., & Harning, R. (2006). An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. The journal of sexual medicine, 3(4), 628-638. ↩︎
Schiöth, H. B., Muceniece, R., Mutulis, F., Prusis, P., Lindeberg, G., Sharma, S. D., & Wikberg, J. E. (1997). Selectivity of cyclic [D-Nal 7] and [D-Phe 7] substituted MSH analogues for the melanocortin receptor subtypes. Peptides,18(7), 1009-1013. ↩︎
King, S.H.; Mayorov AV; Balse-Srinivasan P; Hruby VJ; Vanderah TW; Wessells H. (2007).”Melanocortin Receptors, Melanotropic Peptides and Penile Erection”. Curr Top Med Chem. 7(11): 1098–1106. ↩︎
Brito, M. N., Brito, N. A., Baro, D. J., Song, C. K., & Bartness, T. J. (2007). Differential activation of the sympathetic innervation of adipose tissues by melanocortin receptor stimulation. Endocrinology, 148(11), 5339-5347. ↩︎
Vergoni, A. V., & Bertolini, A. (2000). Role of melanocortins in the central control of feeding. European journal of pharmacology, 405(1), 25-32. ↩︎
Chen, A. S., Metzger, J. M., Trumbauer, M. E., Guan, X. M., Yu, H., Frazier, E. G., & Van der Ploeg, L. H. (2000). Role of the melanocortin-4 receptor in metabolic rate and food intake in mice. Transgenic research, 9(2), 145-154. ↩︎
Wessells, H., Fuciarelli, K., Hansen, J., Hadley, M. E., Hruby, V. J., Dorr, R., & Levine, N. (1998). Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study. The Journal of urology, 160(2), 389-393. ↩︎

All literature, information, and data, provided on this website are for informational and educational purposes only.

Molecular Formula	C₅₀H₆₈N₁₄O₁₀
Molecular Weight	1025.2
Monoisotopic Mass	1024.52428442
Polar Area	379
Complexity	1950
XLogP	0.7
Heavy Atom Count	74
Hydrogen Bond Donor Count	13
Hydrogen Bond Acceptor Count	12
Rotatable Bond Count	17
Physical Appearance	Fine White Lyophilized Powder
Stability	Lyophilized protein is to be stored at -20°C. It is recommended to aliquot the reconstituted (dissolved) protein into several discrete vials in order to avoid repeated freezing and thawing. Reconstituted protein can be stored at 4°C
PubChem LCSS	PT-141 (Bremelanotide) Laboratory Chemical Safety Summary

Property	Property Value
CID	9941379
CAS	189691-06-3
InChI	InChI=1S/C50H68N14O10/c1-3-4-16-35(58-29(2)65)43(67)64-41-25-42(66)54-20-11-10-18-37(49(73)74)60-46(70)39(23-31-26-56-34-17-9-8-15-33(31)34)62-44(68)36(19-12-21-55-50(51)52)59-45(69)38(22-30-13-6-5-7-14-30)61-47(71)40(63-48(41)72)24-32-27-53-28-57-32/h5-9, 13-15, 17, 26-28, 35-41, 56H, 3-4, 10-12, 16, 18-25H2, 1-2H3, (H, 53, 57)(H, 54, 66)(H, 58, 65)(H, 59, 69)(H, 60, 70)(H, 61, 71)(H, 62, 68)(H, 63, 72)(H, 64, 67)(H, 73, 74)(H4, 51, 52, 55)/t35-, 36-, 37-, 38+, 39-, 40-, 41-/m0/s1
InChIKey	FFHBJDQSGDNCIV-MFVUMRCOSA-N
Isomeric SMILES	CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)O)NC(=O)C
Canonical SMILES	CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)O)NC(=O)C
IUPAC Name	(3S, 6S, 9R, 12S, 15S, 23S)-15-[[(2S)-2-acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-2, 5, 8, 11, 14, 17-hexaoxo-1, 4, 7, 10, 13, 18-hexazacyclotricosane-23-carboxylic acid

PT-141 (Bremelanotide)

Properties

Identifiers

2D Structure

Description

Product Comparison

Synonyms:

Peer-Reviewed Sources: